| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| PF 431396 | Axon 2107
CAS [717906-29-1]
MF C22H21F3N6O3SMW 506.50
Purity:
99%
Soluble in DMSO
Description
Dual focal adhesion kinase (FAK or PTK2) and proline-rich tyrosine kinase 2 (PYK2) inhibitor, with high affinity IC50 values of 1.5 nM and 11 nM for FAK and PYK2 respectively; PF 431396 increases bone formation and protects against bone loss in ovariectomized rats
References
Certificates
Categories
Extra info
L Buckbinder et al. Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis. Proc. Nat. Acad. Sci. 2007, 104(25), 10619-10624.
S Han et al. Structural characterization of proline-rich tyrosine kinase 2 (PYK2) reveals a unique (DFG-out) conformation and enables inhibitor design. J. Biol. Chem. 2009, 19, 13193-13201.
DP Walker et al. Sulfoximine-substituted trifluoromethylpyrimidine analogs as inhibitors of proline-rich tyrosine kinase 2 (PYK2) show reduced hERG activity. Bioorg. Med. Chem. Let. 2009, 19(12), 3253-3258.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
FAK
PYK2
MAPK
EC 2.7.10.2
Pfizer Licensed Products
Dual FAK(PTK2) and PYK2 inhibitor
Chemical name
N-methyl-N-(2-((2-(2-oxoindolin-5-ylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)phenyl)methanesulfonamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[717906-29-1]
Order
Size
Unit Price
Stock
5 mg
€80.00
In Stock | | axonmedchem |
| PF 573228 | Axon 1623
CAS [869288-64-2]
MF C22H20F3N5O3SMW 491.49
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of focal adhesion kinase (FAK) with IC50 of 4 nM; Displays 50-250-fold selectivity over other protein kinases; a useful tool in functional study of non-receptor tyrosine inhibitor FAK in integrin-dependent signaling pathways in normal and cancer cells
References
Certificates
Categories
Extra info
ML Jones et al. Characterization of a novel focal adhesion kinase inhibitor in human platelets. Biochem Biophys Res Commun. 2009, 389(1), 198-203.
JK Slack-Davis et al. Cellular Characterization of a Novel Focal Adhesion Kinase Inhibitor. J. Biol. Chem. 2007, 282, 14845-14852.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
FAK
EC 2.7.10.2
FAK inhibitor
Chemical name
6-(4-(3-(methylsulfonyl)benzylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-3,4-dihydroquinolin-2(1H)-one
Parent CAS No.
[869288-64-2]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| IACS-010759 - IACS-10759 | Axon 2909
CAS [1570496-34-2]
MF C25H25F3N6O4SMW 562.56
Purity:
99%
Soluble in DMSO
Description
IACS-010759 is an orally bioavailable, potent inhibitor of complex I of oxidative phosphorylation (OXPHOS). IACS-010759 was active in mouse, rat and cynomolgus monkey with IC50 values of 5.6 nM, 12.2 nM and 8.7 nM, respectively. Treatment with IACS-010759 robustly inhibited proliferation and induced apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS, likely owing to a combination of energy depletion and reduced aspartate production that leads to impaired nucleotide biosynthesis.
KEYWORDS: IACS-010759 | supplier | OxPhos inhibitor | IACS-10759 | IACS 010759 | IACS010759 | IACS 10759 | IACS10759 | CAS [1570496-34-2] | NADH | NADH dehydrogenase | Inhibitor | Enzymes | OxPhos | Complex I | Brain cancer | AML | | axonmedchem |
| GSK837149 | Axon 2617
CAS [13616-29-0]
MF C23H22N8O5S2MW 554.60
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Selective inhibitor of human fatty acid synthase (FAS; Ki value 30 nM) that acts by inhibition the β-ketoacyl reductase activity of the enzyme.
KEYWORDS: GSK837149 | supplier | FAS inhibitor | GSK 837149A | GSK-837149A | CAS [13616-29-0] | Fatty acid synthase | FASN | lipids | beta-ketoacyl reductase | KR | CoA | prostate | ovarian | cancer | carcinoma | obesity | | axonmedchem |
| TH 5487 | Axon 2934
CAS [2304947-71-3]
MF C19H18BrIN4O2MW 541.18
Purity:
98%
Soluble in DMSO
Recently added | | axonmedchem |
| LIMK1 inhibitor BMS 4 - BMS 4 | Axon 1949
CAS [905298-84-2]
MF C23H23N7O2SMW 461.54
Purity:
99%
Soluble in DMSO
Description
A potent LIM kinase 1 (LIMK1; IC50 22nM) inhibitor, devoid of any off-target cytotoxic effects
References
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Extra info
BE Sleebs et al. De Novo Synthesis of a Potent LIMK1 Inhibitor. Synthesis 2010, 7, 1091-1096.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
EC 2.7.11.1
LIMK
LIM Kinase 1 (LIMK1) inhibitor
Chemical name
1-ethyl-3-(5-(6-(4-methoxy-2,6-dimethylphenyl)-2-(pyrazin-2-yl)pyrimidin-4-yl)thiazol-2-yl)urea
Parent CAS No.
[905298-84-2]
Order
Size
Unit Price
Stock
2 mg
€105.00
In Stock | | axonmedchem |
| Miglitol | Axon 2067
CAS [72432-03-2]
MF C8H17NO5MW 207.22
Purity:
98%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
α-glucosidase inhibitor; an oral anti-diabetic drug
References
Certificates
Categories
Extra info
S. Minatoguchi et al. A novel anti-diabetic drug, miglitol, markedly reduces myocardial infarct size in rabbits. Br. J. Pharmacol. 1999, 128, 1667-1672.
Certificate of Analysis
Material Safety Data Sheet
Diabetes & Metabolism
Glucosidase-α
EC 3.2.1.20
Pfizer Licensed Products
α-glucosidase inhibitor; oral anti-diabetic
Chemical name
(2R,3R,4R,5S)-1-(2-hydroxyethyl)-2-(hydroxymethyl)piperidine-3,4,5-triol
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[72432-03-2]
Order
Size
Unit Price
Stock
10 mg
€55.00
In Stock | | axonmedchem |
| Kifunensine, (+)- - FR 900494 | Axon 1730
CAS [109944-15-2]
MF C8H12N2O6MW 232.19
Purity:
99%
Soluble in water and DMSO
Description
A potent class I α-mannosidase inhibitor that inhibits the glycoprotein biosynthesis; inhibits both human endoplasmic reticulum α-mannosidase I and Golgi class I mannosidase with Ki value of 130 and 23 nM respectively
References
Certificates
Categories
Extra info
H Kayakiri et al. Structure of kifunensine, a new immunomodulator isolated from an actinomycete. J. Org. Chem. 1989, 54(17), 4015-4016.
AD Elbein et al. Kifunensine, a potent inhibitor of the glycoprotein processing mannosidase I. J. Biol. Chem. 1990, 265(26), 15599-15605.
KW Hering et al. A practical synthesis of kifunensine analogues as inhibitors of endoplasmic reticulum alpha-mannosidase I. J Org Chem. 2005, 70(24), 9892-9904.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
Mannosidase-α
EC 3.2.1.24
α-mannosidase inhibitor
Chemical name
(5R,6R,7S,8R,8aS)-6,7,8-trihydroxy-5-(hydroxymethyl)tetrahydroimidazo[1,2-a]pyridine-2,3(1H,5H)-dione
Parent CAS No.
[109944-15-2]
Order
Size
Unit Price
Stock
2 mg
€120.00
In Stock | | axonmedchem |
| T56-LIMKi - T5601640 | Axon 2721
CAS [924473-59-6]
MF C19H14F3N3O3MW 389.33
Purity:
99%
Soluble in DMSO
Description
T56-LIMKi is an inhibitor of LIMK2. T56-LIMKi efficiently inhibited the growth of NF1-/- MEF, ST88-14, U87, and Panc-1 cells with IC50 values of 30 μM, 18 μM, 7 μM, and 35 μM, respectively. Moreover, T56-LIMKi reduced tumor size and p-cofilin levels in the Panc-1 tumors in vivo. Potential drug for pancreatic cancer, glioma and schwannoma cells.
KEYWORDS: T56-LIMKi | supplier | LIMK2 inhibitor | T5601640 | T56 LIMKi | T56LIMKi | T 5601640 | T-5601640 | CAS [924473-59-6] | Non Selective (ADF-cofilin) | LIMK2 | Inhibitor | Enzymes | LIM | LIM kinase | cofilin | ADF | Panc-1 | | axonmedchem |
| Lalistat 2 | Axon 2797
CAS [1234569-09-5]
MF C13H20N4O2SMW 296.39
Purity:
99%
Soluble in DMSO
Description
Lalistat 2 is a potent and selective inhibitor of lysosomal acid lipase (LAL) with an IC50 value of 152 nM. Lalistat 2 did not exhibit inhibition of human pancreatic lipase or bovine milk lipoprotein lipase.
KEYWORDS: Lalistat 2 | supplier | LAL inhibitor | Lalistat2 | Lalistat-2 | CAS [1234569-09-5] | Triglycerides | LAL | Inhibitor | Enzymes | Niemann-Pick type C | | axonmedchem |
| MALT1 inhibitor MI-2 | Axon 2054
CAS [1047953-91-2]
MF C19H17Cl3N4O3MW 455.72
Purity:
100%
Soluble in DMSO
Description
Highly potent and selective MALT1 inhibitor; MI-2 binds directly to MALT1 and suppresses activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) in vitro and in vivo. MI-2 is notably nontoxic to mice
References
Certificates
Categories
Extra info
L Fontan et al. MALT1 small molecule inhibitors specifically suppress ABC-DLBCL in vitro and in vivo. Cancer Cell. 2012, 22(6), 812-24.
RM Young & LM Staudt. A New “Brew” of MALT1 Inhibitors. Cancer Cell, 2012, 22(6), 706-707.
DJ Burgess. Anticancer drugs: Assault on MALT1. Nature Reviews Drug Discovery, 2013, 12(2), 100-101.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
Pain & Inflammation
MALT1
NF-κB
EC 3.4.22
Highly potent and selective MALT1 inhibitor
Chemical name
2-chloro-N-(4-(5-(3,4-dichlorophenyl)-3-(2-methoxyethoxy)-1H-1,2,4-triazol-1-yl)phenyl)acetamide
Parent CAS No.
[1047953-91-2]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| NCL-00017509 | Axon 2728
CAS [1507367-00-1]
MF C15H12N6OMW 292.30
Purity:
100%
Soluble in DMSO
Description
NCL-00017509 is a potent kinase-selective irreversible Nek2 inhibitor (IC50 value of 56 nM) with promising drug-like properties.
KEYWORDS: NCL-00017509 | supplier | Nek2 Inhibitor | NCL00017509 | NCL 00017509 | CAS [1507367-00-1] | C-Nap1 | PP1 | Nek2 | Nek | Inhibitor | Enzymes | | axonmedchem |
| Thioridazine hydrochloride | Axon 2193
CAS [130-61-0]
MF C21H26N2S2.HClMW 407.04
Purity:
99%
Soluble in water and DMSO
Description
Antipsychotic with (sub-) nanomolar affinity for dopamine and α-adrenergic receptors (Ki of 0.4 nM, 1.5 nM, 1.5 nM, 3.2 nM, 2.4 nM for D2, D3, D4, α1A, and α1B resp.).
Recently, Thioridazine was found to inhibit full length recombinant MALT1 (IC50 3.43 μM). It inhibits anti-apoptotic NF-κB signaling and elicits toxic effects selectively on MALT1-dependent ABC-DLBCL cells. Additionally, it suppresses tumor growth activity by targeting the PI3K/Akt/mTOR/p70S6K signaling pathway.
References
Certificates
Categories
Extra info
D. Nagel et al. Pharmacologic Inhibition of MALT1 Protease by Phenothiazines as a Therapeutic Approach for the Treatment of Aggressive ABC-DLBCL. Canc. Cell 2012, 22, 825–837.
S. Kang et al. Thioridazine induces apoptosis by targeting the PI3K/Akt/mTOR pathway in cervical and endometrial cancer cells. Apoptosis. 2012, 17, 989–997.
RM Young & LM Staudt. A New “Brew” of MALT1 Inhibitors. Cancer Cell, 2012, 22(6), 706-707.
DJ Burgess. Anticancer drugs: Assault on MALT1. Nature Reviews Drug Discovery, 2013, 12(2), 100-101.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
CNS
D2
D3
D4
Adrenoceptor α1
MALT1
NF-κB
PI3K-Akt-mTOR
EC 3.4.22
Stem Cell Differentiator
DA and α1 adrenoceptor antagonist; MALT1 inhibitor
Chemical name
10-(2-(1-methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine hydrochloride
Parent CAS No.
[50-52-2]
Order
Size
Unit Price
Stock
10 mg
€50.00
In Stock | | axonmedchem |
| NVP 231 | Axon 1600
CAS [362003-83-6]
MF C25H25N3O2SMW 431.55
Purity:
99%
Soluble in DMSO and Ethanol
Description
Potent, specific and reversible ceramide kinase (CerK) inhibitor with activity in low nanomolar range
References
Certificates
Categories
Extra info
C Graf et al. Targeting ceramide metabolism with a potent and specific ceramide kinase inhibitor. Mol. Pharmacol. 2008, 74(4), 925-932.
C Graf et al. A secondary assay for ceramide kinase inhibitors based on cell growth inhibition by short-chain ceramides. Anal. Biochem. 2009, 384(1), 166-169.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CerK
EC 2.7.1.138
CerK inhibitor
Chemical name
Adamantane-1-carboxylic acid (2-benzoylamino-benzothiazol-6-yl)amide
Parent CAS No.
[362003-83-6]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| PluriSIn #1 - NSC 14613 | Pluripotent cell-specific inhibitor #1 | Axon 2091
CAS [91396-88-2]
MF C12H11N3OMW 213.24
Purity:
99%
Soluble in DMSO and Ethanol
Description
An inhibitor of stearoyl-coA desaturase (SCD1), the key enzyme in oleic acid biosynthesis; a pluripotent cell-specific inhibitor (PluriSIn) used to selectively eliminate undifferentiated human pluripotent stem cells (hPSCs)
References
Certificates
Categories
Extra info
U Ben-David et al. Selective elimination of human pluripotent stem cells by an oleate synthesis inhibitor discovered in a high-throughput screen. Cell Stem Cell. 2013, 12(2), 167-179.
Certificate of Analysis
Material Safety Data Sheet
Diabetes & Metabolism
Stem Cell
SCD1
EC 1.14.19.1
Stem Cell Differentiator
Inhibitor of stearoyl-coA desaturase (SCD1)
Chemical name
N'-phenylisonicotinohydrazide
Parent CAS No.
[91396-88-2]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| SB 747651A - SB 747651 tetrahydrochloride | Axon 1897
CAS [N.A.]
MF C16H22N8O.4HClMW 488.24
Purity:
98%
Soluble in water and DMSO
Description
Potent MSK inhibitor; In vitro, SB-747651A inhibits MSK1 with an IC50 value of 11 nM; In cells, SB-747651A fully inhibited MSK activity at 5-10 μM.SB-747651A exhibited improved selectivity over H89 and Ro 31-8220 and therefore represents a useful tool to study MSK function in cells
References
Certificates
Categories
Extra info
S Naqvi et al. Characterization of the cellular action of the MSK inhibitor SB-747651A. Biochem J. 2012, 441(1), 347-357.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
MSK1
MAPK
EC 2.7.11.1
Inhibitor of MSK1
Chemical name
4-(1-ethyl-7-((piperidin-4-ylamino)methyl)-1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-amine tetrahydrochloride
Parent CAS No.
[607372-46-3]
Order
Size
Unit Price
Stock
5 mg
€120.00
In Stock | | axonmedchem |
| STX64 - BN83495 | Irosustat | 667 Coumate | Axon 2892
CAS [288628-05-7]
MF C14H15NO5SMW 309.34
Purity:
99%
Soluble in DMSO
Description
Potent steroid sulfatase (STS) inhibitor with an IC50 value of 8 nM. First STS inhibitor to enter diverse clinical trials for patients with advanced hormone-dependent cancer.
Keywords: STX64 | supplier | STS inhibitor | BN83495 | Irosustat | 667 Coumate | STX 64 | STX-64 | BN 83495 | BN-83495 | CAS [288628-05-7] | Steroids | STS | Inhibitor | Enzymes | Steryl-sulfatase | Arylsulfatase C | Estrone sulfatase | | axonmedchem |
| STK16-IN-1 | Axon 2743
CAS [1223001-53-3]
MF C17H12FN3OMW 293.30
Purity:
99%
Soluble in DMSO
Description
STK16-IN-1 is a highly selective ATP-competitive inhibitor which exhibits potent inhibitory activity against STK16 kinase (IC50 value of 0.295 μM). In MCF-7 cells, treatment with STK16-IN-1 results in a reduction in cell number and accumulation of binucleated cells, which can be recapitulated by RNAi knockdown of STK16. Co-treatment of STK16-IN-1 with chemotherapeutics results in a slight potentiation of the antiproliferative effects of the chemotherapeutics.
References
Certificates
Categories
Extra info
F Liu et al. Discovery of a Highly Selective STK16 Kinase Inhibitor. ACS Chem Biol. 2016 Jun 17;11(6):1537-43.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
EC 2.7.10.2
STK16
ATP-competitive STK16 inhibitor
Chemical name
1-(4-Fluoro-3-methylphenyl)-1H-pyrrolo[2,3-h][1,6]naphthyridin-2(7H)-one
Parent CAS No.
[1223001-53-3]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| WNK Inhibitor 11 | Axon 2896
CAS [2123489-30-3]
MF C21H21Cl2N5OSMW 462.40
Purity:
98%
Soluble in DMSO
Description
Selective allosteric WNK1 inhibitor (IC50 value of 0.004 µM) with nearly 1000-fold selectivity for WNK1 vs WNK4 and 57-fold selectivity for WNK1 vs WNK2.
Keywords: WNK Inhibitor 11 | supplier | WNK1 inhibitor | CAS [2123489-30-3] | Cation-Cl− cotransporters (CCCs) | WNK | Inhibitor | Enzymes | Hypertension | | axonmedchem |
| CP 316819 | Axon 1847
CAS [186392-43-8]
MF C21H22ClN3O4MW 415.87
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent glycogen phosphorylase (GPase) inhibitor (IC50: 40 nM against human liver GPα). CP-316819 facilitates glycogen utilization in the brain, prevents neuronal cell death and maintains brain electrical currents
References
Certificates
Categories
Extra info
SW Suh et al. Astrocyte glycogen sustains neuronal activity during hypoglycemia: studies with the glycogen phosphorylase inhibitor CP-316,819 ([R-R*,S*]-5-chloro-N-[2-hydroxy-3-(...). J. Pharmacol. Exp. Ther. 2007, 1, 45-50.
DG Baker et al. Glycogen phosphorylase inhibition in type 2 diabetes therapy: a systematic evaluation of metabolic and functional effects in rat skeletal muscle. Diabetes 2005, 54, 2453.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
GPase
EC 2.4.1.1
Glycogen Phosphorylase (GPase) inhibitor
Chemical name
5-chloro-N-((2S,3R)-3-hydroxy-4-(methoxy(methyl)amino)-4-oxo-1-phenylbutan-2-yl)-1H-indole-2-carboxamide
Parent CAS No.
[186392-43-8]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| BEC hydrochloride - S-(2-Boronoethyl)-L-cysteine hydrochloride | Axon 2373
CAS [222638-67-7]
MF C5H12BNO4S.HClMW 229.49
Purity:
99%
Soluble in water and DMSO
Description
Slow-binding pH-dependent inhibitior of human Arginase I and II (Kd value 270 nM and 220 nM for Arginase I and II, respectively. Ki values 310 nM and 30 nM at pH 7.5 and pH 9.5, respectively for Arginase II). Valuable reagent to probe the physiological relationship between arginase and nitric oxide (NO) synthase in regulating the NO-dependent smooth muscle relaxation in human penile corpus cavernosum tissue. BEC Does not inhibit NO synthase, and effectively prevented ACh tolerance in aortic and mesenteric artery preparations.
KEYWORDS: BEC hydrochloride | supplier | Arginase inhibitor | S-(2-Boronoethyl)-L-cysteine hydrochloride | CAS [222638-67-7] | [63107-40-4] | Axon Medchem | Axon 2373 | Arginine | Arginase | Arginase II | Arginase I | Arginemia | NO | penile | sexual | dysfunction | ureagenesis | Arginine | urea cycle | Ornithine cycle | Inhibitor | Enzymes | | axonmedchem |
| BCI-121 | Axon 2735
CAS [432529-82-3]
MF C14H18BrN3O2MW 340.22
Purity:
99%
Soluble in DMSO
Description
BCI-121 induces a significant reduction in SMYD3 activity both in vitro and in CRC cells, as suggested by the analysis of global H3K4me2/3 and H4K5me levels. Moreover, BCI-121 inhibits chromatin recruitment and is effective in reducing proliferation in various cancer cell types.
KEYWORDS: BCI-121 | supplier | SMYD3 inhibitor | BCI 121 | BCI121 | CAS [432529-82-3] | Histone | HMTase | Inhibitor | Enzymes | | axonmedchem |
| A 357300 hydrochloride | Axon 1666
CAS [369358-07-6]
MF C15H22ClN3O3S.HClMW 396.33
Purity:
100%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and reversible inhibitor of methionine aminopeptidase-2 (MetAP-2)
References
Certificates
Categories
Extra info
J Wang et al. Tumor suppression by a rationally designed reversible inhibitor of methionine aminopeptidase-2. Cancer Res. 2003, 63(22), 7861-7869.
MJ Morowitz et al. Methionine aminopeptidase 2 inhibition is an effective treatment strategy for neuroblastoma in preclinical models. Clin. Cancer Res. 2005, 11(7), 2680-2685.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cardiovascular
Cell Signaling & Oncology
MetAP2
EC 3.4.11.18
MetAP2 inhibitor
Chemical name
N'-((2S,3R)-3-amino-2-hydroxy-5-(isopropylthio)pentanoyl)-3-chlorobenzohydrazide hydrochloride
Parent CAS No.
[369358-07-6]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| Naltrexone hydrochloride - NIH 8503 | Axon 2416
CAS [16676-29-2]
MF C20H23NO4.HClMW 377.86
Purity:
100%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
Competitive opioid antagonist with preference for µ- and κ-receptors over δ-receptor (Ki values 1.55 nM, 7.84 nM, and 0.71 nM for µ-, δ-, and κ-receptors, respectively)
References
Certificates
Categories
Extra info
K. Uwai et al. Syntheses and receptor-binding studies of derivatives of the opioid antagonist naltrexone. Bioorg Med Chem. 2004 Jan 15;12(2):417-21.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
Endocrinology
OPR-κ
OPR-μ
OPR-δ
A4
Competitive opioid antagonist with preference for µ- and κ-receptors
Chemical name
(5α)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-morphinan-6-one hydrochloride
Parent CAS No.
[16590-41-3]
Order
Size
Unit Price
Stock
50 mg
€45.00
In Stock | | axonmedchem |
| Naloxone hydrochloride - NIH 7890 | Narcan | Axon 2415
CAS [357-08-4]
MF C19H21NO4.HClMW 363.84
Purity:
99%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
Neutral opioid antagonist (Ki values 0.81 nM and 1.80 nM for µ- and δ-opioid, respectively)
References
Certificates
Categories
Extra info
D. Wang et al. Inverse agonists and neutral antagonists at mu opioid receptor (MOR): possible role of basal receptor signaling in narcotic dependence. J Neurochem. 2001 Jun;77(6):1590-600.
S.M. Hölter et al. Effects of opiate antagonist treatment on the alcohol deprivation effect in long-term ethanol-experienced rats. Psychopharmacology (Berl). 1999 Aug;145(4):360-9.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
Endocrinology
OPR-μ
OPR-δ
A4
Neutral opioid antagonist
Chemical name
(5α)-4,5-epoxy-3,14-dihydroxy-17-(2-propen-1-yl)-morphinan-6-one hydrochloride
Parent CAS No.
[465-65-6]
Order
Size
Unit Price
Stock
50 mg
€45.00
In Stock | | axonmedchem |
| Naloxone Benzoylhydrazone | Axon 1230
CAS [119630-94-3]
MF C26H27N3O4MW 445.51
Purity:
98%
Soluble in DMSO
Description
Agonist for κ3 opioid receptors; antagonist for ORL1 and μ opioid receptors
References
Certificates
Categories
Extra info
MA Gistrak et al. Pharmacological actions of a novel mixed opiate agonist/antagonist: Naloxone benzoylhydrazone. J. Pharmacol. Exp. Ther. 1989, 251, 469-476.
D Paul et al. Naloxone benzoylhydrazone (NalBzoH) analgesia. J. Pharmacol. Exp. Ther. 1990, 255, 769-774.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Pain & Inflammation
Endocrinology
OPR-κ
A4
Kappa-opioid agonist
Chemical name
2-[(5a)-4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)morphinan-6-ylidene]hydrazide benzoic acid
Parent CAS No.
[119630-94-3]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| SB 612111 hydrochloride | Axon 1413
CAS [371980-98-2]
MF C24H29ClNO.HClMW 454.86
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Selective NOP receptor antagonist
References
Certificates
Categories
Extra info
Anna Rizzi et al. Pharmacological Characterization of the Nociceptin/Orphanin FQ Receptor Antagonist SB-612111: In Vivo Studies. J. Pharmacol. Exp. Ther. 2007, 321(3), 968-974.
B Spagnolo et al. Pharmacological characterization of the nociceptin/orphanin FQ receptor antagonist SB-612111: in vitro studies. J Pharmacol. Exp. Ther. 2007, 321(3), 961-7.
PF Zaratin et al. Modification of nociception and morphine tolerance by the selective opiate receptor-like orphan receptor antagonist SB-612111. J. Pharmacol. Exp. Ther. 2004, 308(2), 454-61.
Certificate of Analysis
Material Safety Data Sheet
CNS
Endocrinology
OPR (NOP)
A4
NOP antagonist
Chemical name
(5S,7S)-7-[4-(2,6-Dichloro-phenyl)-piperidin-1-ylmethyl]-1-methyl-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol hydrochloride
Parent CAS No.
[371980-98-2]
Order
Size
Unit Price
Stock
2 mg
€70.00
In Stock | | axonmedchem |
| SNC 80 | Axon 1412
CAS [156727-74-1]
MF C28H39N3O2MW 449.63
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq)
Description
Selective and potent δ opioid receptor agonist.
KEYWORDS: SNC 80 | δ-opioid agonist | SNC80 | CAS [156727-74-1] | Opioids | OPR-δ | Agonist | Receptors | | axonmedchem |
| U 50488 hydrochloride | Axon 1202
CAS [109620-49-7]
MF C19H26Cl2N2O.HClMW 405.79
Purity:
99%
Optical purity:
>98% ee
Soluble in water
Description
Selective nonpeptide kappa-Opioid receptor agonist, which has been found to stimulate the release of adrenocorticotropin (acth) via the release of hypothalmic arginine vasopressin and corticotropin releasing factor
References
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ML Laorden et al. Effects of U-50,488H and U-50,488H withdrawal on c-fosexpression in the rat paraventricular nucleus. Correlation with c-fos in brainstem catecholaminergic neurons. Br. J. Pharmacol. 2003, 138, 1544–1552.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Pain & Inflammation
Endocrinology
OPR-κ
A4
Kappa-opioid agonist
Chemical name
2-(3,4-Dichloro-phenyl)-N-methyl-N-((R)-2-pyrrolidin-1-yl-cyclohexyl)-acetamide hydrochloride (racemic)
Parent CAS No.
[67198-13-4]
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Size
Unit Price
Stock
10 mg
€65.00
In Stock | | axonmedchem |
| Naloxonazine dihydrochloride - NSC 612113 | Axon 1205
CAS [880759-65-9]
MF C38H42N4O6.2HClMW 723.69
Purity:
97%
Soluble in water
Description
Opioid receptor antagonist
References
Certificates
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Extra info
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Pain & Inflammation
Endocrinology
OPR-μ
A4
Opioid antagonist
Chemical name
4,5-epoxy-3,14-dihydroxy-17-(2-propen-1-yl)-, 2-[(5a)-4,5-epoxy-3,14-dihydroxy-17-(2-propen-1-yl)morphinan-6-ylidene]hydrazone-morphinan-6-one dihydrochloride
Parent CAS No.
[82824-01-9]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| Nalmefene hydrochloride | Axon 1573
CAS [58895-64-0]
MF C21H25NO3.HClMW 375.89
Purity:
99%
Soluble in water and DMSO
Description
Non selective opioid receptor antagonist; it acts by blocking a mechanism in the brain that can cause a continuing and uncontrolled intake of alcohol. This helps to control and reduce alcohol intake
References
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Extra info
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
Endocrinology
OPR-κ
OPR-μ
OPR-δ
A4
Opioid antagonist
Chemical name
17-cyclopropylmethyl-4,5α-epoxy-6-methylenemorphinan-3,14-diol
Parent CAS No.
[55096-26-9]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| Nalbuphine hydrochloride | Axon 1577
CAS [23277-43-2]
MF C21H27NO4.HClMW 393.90
Purity:
99%
Soluble in water
Description
A narcotic used as a pain medication. Nalbuphine appears to be an agonist at κ-opioid receptors and an antagonist or partial agonist at μ-opioid receptors (IC50 of 36 nM and 11 nM resp).
References
Certificates
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Extra info
P Gharagozlou et al. Activity of opioid ligands in cells expressing cloned µ opioid receptors. B.M.C. Pharmacol. 2003, 3, 1-8.
K Yasuda et al. Cloning and functional comparison of kappa and delta opioid receptors from mouse brain. Proc. Natl. Acad. Sci. USA. 1993, 90, 6736-6740.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Pain & Inflammation
Endocrinology
OPR-κ
A4
Analgesic. Κ-opioid agonist and μ-opioid antagonist/partial agonist
Chemical name
(–)-17-(cyclobutylmethyl)- 4,5α-epoxymorphinan- 3,6α,14-triol Hydrochloride
Parent CAS No.
[20594-83-6 ]
Order
Size
Unit Price
Stock
10 mg
€110.00
In Stock | | axonmedchem |
| JTC 801 | Axon 1805
CAS [244218-51-7 ]
MF C26H25N3O2.HClMW 447.96
Purity:
98%
Soluble in DMSO
Description
Potent and selective NOP receptor antagonist (Ki: 8.2 nM)
References
Certificates
Categories
Extra info
H Yamada et al. Pharmacological profiles of a novel opioid receptor-like1 (ORL1) receptor antagonist, JTC-801. Br. J. Pharmacol. 2002, 135, 323.
H Tamai et al. Anti-allodynic and anti-hyperalgesic effects of nociceptin receptor antagonist, JTC-801, in rats after spinal nerve injury and inflammation. Eur. J. Pharmacol. 2005, 510, 223.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
Endocrinology
OPR (NOP)
A4
NOP receptor antagonist
Chemical name
N-(4-amino-2-methylquinolin-6-yl)-2-((4-ethylphenoxy)methyl)benzamide hydrochloride
Parent CAS No.
[244218-93-7]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| HS666 hydrochloride | Axon 2781
CAS [1409931-99-2]
MF C20H25NO.HClMW 331.88
Purity:
99%
Soluble in DMSO
Description
HS666 is a selective κ opioid receptor partial agonist (Ki value of 5.9 nM) which activates central κ receptors to produce potent antinociception. Moreover, HS666 displays pharmacological characteristics of a κ receptor analgesic with reduced liability for aversive effects correlating with its low efficacy in the β-arrestin2 signalling pathway.
Keywords: HS666 hydrochloride | supplier | Kappa-opioid partial agonist | HS 666 hydrochloride | HS-666 hydrochloride | CAS [1409931-99-2] | [1409931-91-4] | Opioids | OPR-κ | Partial agonist | Receptors | Antinociception | | axonmedchem |
| GNTI dihydrochloride - Guanidinonaltrindole dihydrochloride, 6'- | Axon 1226
CAS [351183-88-5]
MF C27H29N5O3.2HClMW 544.47
Purity:
99%
Soluble in water and DMSO
Description
Kappa opioid antagonist.
KEYWORDS: GNTI dihydrochloride | supplier | Kappa-opioid antagonist | Guanidinonaltrindole dihydrochloride, 6'- | GNTI | CAS [351183-88-5] | [219655-56-8] | Opioids | OPR-κ | Antagonist | Receptors | | axonmedchem |
| Funaltrexamine hydrochloride, β- - FNA hydrochloride, β- | Axon 1213
CAS [72786-10-8]
MF C25H30N2O6.HClMW 490.98
Purity:
98%
Soluble in water and DMSO
Description
Selective irreversible μ opioid receptor antagonist
References
Certificates
Categories
Extra info
JH Broadbear et al. Methocinnamox is a potent long-lasting and selective antagonist of morphine-mediated antinociception in the mouse: comparison with clocinnamox, beta-funaltrexamine and beta-chlornaltrexamine. J. Pharmacol. Exp. Ther. 2000, 294, 933.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
Endocrinology
OPR-μ
A4
Mu-opioid antagonist
Chemical name
(2E)-4-[[(5a,6b)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]amino]-4-oxo-2-Butenoic acid methyl ester, hydrochloride (1:1)
Parent CAS No.
[72782-05-9]
Order
Size
Unit Price
Stock
2 mg
€90.00
In Stock | | axonmedchem |
| Fedotozine tartrate - JO 1196 | Axon 1140
CAS [133267-27-3]
MF C22H31NO4.C4H6O6MW 523.57
Purity:
99%
Optical purity:
99% ee
Soluble in water
Description
kappa(1a) opioid receptor agonist
References
Certificates
Categories
Extra info
M Delvaux. Pharmacology and clinical experience with fedotozine. Expert Opin. Investig. Drugs 2001, 10(1), 97-110.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
Endocrinology
OPR-κ
A4
Kappa(1a) opioid agonist
Chemical name
Dimethyl-[(R)-1-phenyl-1-(3,4,5-trimethoxy-benzyloxymethyl)-propyl]-amine tartrate
Parent CAS No.
[123618-00-8]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| Binaltorphimine dihydrochloride, nor- | Axon 1163
CAS [113158-35-3]
MF C40H43N3O6.2HClMW 734.71
Purity:
98%
No solubility data
Description
Potent and selective kappa opioid receptor antagonist
References
Certificates
Categories
Extra info
SD Mague et al. Antidepressant-like effects of kappa-opioid receptor antagonists in the forced swim test in rats. J. Pharmacol Exp. Ther. 2003, 305(1), 323-30.
MJ Picker et al. Opioids and rate of positively reinforced behavior: III. Antagonism by the long-lasting kappa antagonist norbinaltorphimine. Behav Pharmacol 1996, 7(6), 495-504.
CNS
Pain & Inflammation
Endocrinology
OPR-κ
A4
Kappa-opioid antagonist
Chemical name
N.A.
Parent CAS No.
[105618-26-6]
Inquire | | axonmedchem |
| BAN ORL 24 dihydrochloride | Axon 1784
CAS [1401463-54-4]
MF C27H35N3O2.2HClMW 506.51
Purity:
99%
Optical purity:
Optically pure
Soluble in water, DMSO, and Ethanol
Description
Highly potent and selective NOP receptor antagonist (IC50: 0.27 nM); more than 2500 fold selective over other opioid receptors
KEYWORDS: BAN ORL 24 | supplier | NOP antagonist | 1401463-54-4 | 475150-69-7 | BANORL24 | BAN-ORL-24 | Opioid | nociceptin | OPR (NOP) | Orphanin | dopamine | D2 | | axonmedchem |
| ADL 5859 | Axon 1751
CAS [850173-95-4]
MF C24H29ClN2O3MW 428.95
Purity:
99%
Soluble in DMSO
Description
Highly potent and selective δ opioid receptor agonist with Ki value to be 0.84 nM and ED50 value to be 20 nM
References
Certificates
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Extra info
B Le Bourdonnec et al. Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide (ADL5859). J. Med. Chem. 2008, 51(19), 5893-5896.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
Endocrinology
OPR-δ
A4
Selective δ-opioid receptor agonist
Chemical name
N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-piperidine]-4-yl)benzamide hydrochloride
Parent CAS No.
[850305-06-5]
Order
Size
Unit Price
Stock
10 mg
€115.00
In Stock | | axonmedchem |
| Osanetant - SR 142801 | Axon 1533
CAS [160492-56-8]
MF C35H41Cl2N3O2MW 606.62
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent non-peptide neurokinin 3 (NK3) receptor antagonist
References
Certificates
Categories
Extra info
X Emonds-Alt et al. SR 142801, the first potent non-peptide antagonist of the tachykinin NK3 receptor. Life Sci. 1995, 56(1), PL27-32.
F Kamali. Osanetant Sanofi-Synthélabo. Curr. Opin. Invest. Drugs. 2001, 2(7), 950-956.
L Quartara and M Altamura. Tachykinin receptors antagonists: from research to clinic. Curr. Drug Targets. 2006, 7(8), 975-992.
MA De Souza Silva et al. The tachykinin NK3 receptor antagonist SR142801 blocks the behavioral effects of cocaine in marmoset monkeys. Eur. J. Pharmacol. 2006, 536(3), 269-278.
G Jocham et al. Neurokinin receptor antagonism attenuates cocaine's behavioural activating effects yet potentiates its dopamine-enhancing action in the nucleus accumbens core. Eur. J. Neurosci. 2006, 24(6), 1721-1732.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
A9
Tachykinin (NK)
NK3 antagonist
Chemical name
N-(1-{3-[(R)-1-Benzoyl-3-(3,4-dichloro-phenyl)-piperidin-3-yl]-propyl}-4-phenyl-piperidin-4-yl)-N-methyl-acetamide
Parent CAS No.
[160492-56-8]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| Orvepitant maleate - GW 823296B | GW 823296X maleate | Axon 1618
CAS [579475-24-4]
MF C31H35F7N4O2.C4H4O4MW 744.70
Purity:
99%
Optical purity:
>98% ee
Soluble in water and DMSO
Description
Neurokinin-1 (NK1) receptor antagonist; potential therapeutic for the treatment of depression and anxiety diseases
References
Certificates
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Extra info
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
A9
Tachykinin (NK)
NK1 antagonist
Chemical name
(2R,4S)-N-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethyl)-2-(4-fluoro-2-methylphenyl)-N-methyl-4-((S)-6-oxohexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl)piperidine-1-carboxamide maleate
Parent CAS No.
[579475-18-6]
Order
Size
Unit Price
Stock
2 mg
€115.00
In Stock | | axonmedchem |
| Netupitant - Ro 67-31898 | Axon 2499
CAS [290297-26-6]
MF C30H32F6N4OMW 578.59
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Highly selective NK 1 receptor antagonist. Approved drug in combination with Palonosetron (clinically and pharmacologically distinct 5-HT3 receptor antagonist) indicated for the prevention of chemotherapy-induced nausea and vomiting (CINV).
KEYWORDS: Netupitant | supplier | RO 67-31898 | | | axonmedchem |
| GR 159897 | Axon 1119
CAS [158848-32-9]
MF C23H27FN2O2SMW 414.54
Purity:
99%
Optical purity:
98% ee
Soluble in DMSO
Description
Potent and selective non-peptide neurokinin NK2 receptor antagonist
References
Certificates
Categories
Extra info
DM Walsh et al. The anxiolytic-like activity of GR 159897, a non-peptide NK2 receptor antagonist, in rodent and primate models of anxiety. Psychopharmacol. 1995, 121, 186-191.
AWJ Cooper et al. GR 159897 and related analogues as highly potent, orally active non-peptide neurokinin NK2 receptor antagonists. Bioorg. Med. Chem. Lett. 1994, 4(16), 1951.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
A9
Tachykinin (NK)
NK2 antagonist
Chemical name
3-[2-(4-(R)-Benzenesulfinylmethyl-4-methoxy-piperidin-1-yl)-ethyl]-5-fluoro-1H-indole
Parent CAS No.
[158848-32-9]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| Casopitant mesylate - GW 679769B | Axon 1901
CAS [414910-30-8]
MF C30H35F7N4O2.CH4O3SMW 712.72
Purity:
100%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
Potent, selective and orally active neurokinin 1 (NK1) receptor antagonist
References
Certificates
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Extra info
E Minthorn et al. Pharmacokinetics and Brain Penetration of Casopitant, a Potent and Selective Neurokinin-1 Receptor Antagonist, in the Ferret. Drug Metabol. Disp. 2008, 36(9), 1846-1852.
C Ruhlmann and J Herrstedt. Casopitant: a novel NK1-receptor antagonist in the prevention of chemotherapy-induced nausea and vomiting. Ther Clin Risk Manag. 2009, 5, 375–384.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
A9
Tachykinin (NK)
NK1 antagonist
Chemical name
(2R,4S)-4-(4-acetylpiperazin-1-yl)-N-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethyl)-2-(4-fluoro-2-methylphenyl)-N-methylpiperidine-1-carboxamide methanesulfonate
Parent CAS No.
[414910-27-3]
Order
Size
Unit Price
Stock
2 mg
€125.00
In Stock | | axonmedchem |
| Aprepitant | Axon 1486
CAS [170729-80-3]
MF C23H21F7N4O3MW 534.43
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Substance P antagonist (SPA), having effect by blocking the neurokinin 1 (NK1) receptor
References
Certificates
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Extra info
K Ranga and R Krishnan. Clinical experience with substance P receptor (NK1) antagonists in depression. J. Clin. Psychiatry 2002, 63 Suppl 11, 25-9.
AK Majumdar et al. Effects of aprepitant on cytochrome P450 3A4 activity using midazolam as a probe. Clin. Pharmacol. Ther. 2003, 74, 150–156.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
A9
Tachykinin (NK)
Substance P antagonist (SPA); NK1 inhibitor
Chemical name
5-[(2R,3S)-2-[(R)-1-(3,5-Bis-trifluoromethyl-phenyl)-ethoxy]-3-(4-fluoro-phenyl)-morpholin-4-ylmethyl]-2,4-dihydro-[1,2,4]triazol-3-one
Parent CAS No.
[170729-80-3]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| Cambinol - NSC 112546 | Axon 2803
CAS [14513-15-6]
MF C21H16N2O2SMW 360.43
Purity:
99%
Soluble in DMSO
Description
Cambinol inhibits NAD-dependent deacetylase activity of human SIRT1 and SIRT2 (IC50 values of 56 and 59 μM, respectively). Consistent with the role of SIRT1 in promoting cell survival during stress, inhibition of SIRT1 activity with cambinol during genotoxic stress leads to hyperacetylation of key stress response proteins and promotes cell cycle arrest. Cambinol exerts antitumor activity in vitro and in mouse xenograft studies. Moreover, cambinol is an uncompetitive nSMase2 inhibitor (Ki value of 7 μM).
KEYWORDS: Cambinol | supplier | SIRT inhibitor | NSC 112546 | NSC112546 | NSC-112546 | CAS [14513-15-6] | Histone | SIRT | Inhibitor | Enzymes | nSMase2 | | axonmedchem |
| Varenicline dihydrochloride - Chantix | Champix | Axon 1384
CAS [866823-63-4]
MF C13H13N3.HClMW 284.18
Purity:
99%
Soluble in water
Description
Selective α4β2 nicotinic acetylcholine receptor partial agonist; Smoking cessation drug. Available also another drug form, Varenicline tartrate (Axon 2074).
References
Certificates
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Extra info
DE Jorenby et al. Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trial. JAMA 2006, 296 (1), 56–63.
RS Obach et al. Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro. Drug Metab Dispos 2006, 34, 121-30.
Mihalak K.B. et al. Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol Pharmacol. 2006 Sep;70(3):801-805.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
nAChR
Unclassified
Pfizer Licensed Products
Nicotinic acetylcholine receptor agonist
Chemical name
7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino(2,3-h)(3)benzazepine dihydrochloride
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[249296-44-4]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| Varenicline tartrate - Chantix | Champix | CP 526555-18 | Axon 2074
CAS [375815-87-5]
MF C17H19N3O6MW 361.35
Purity:
100%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
Selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist; Smoking cessation drug. Available also another drug form, Varenicline di-HCl (Axon 1384).
References
Certificates
Categories
Extra info
D.E. Jorenby et al. Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trial. JAMA 2006, 296, 56-63.
R.S. Obach et al. Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro. Drug Metab. Dispos. 2006, 34, 121-30.
K.B. Mihalak et al. Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol. Pharmacol. 2006, 70, 801-805.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
nAChR
Unclassified
Pfizer Licensed Products
Selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist
Chemical name
7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino(2,3-h)(3)benzazepine tartrate
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[249296-44-4]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| PNU 282987 hydrochloride | Axon 2908
CAS [123464-89-1]
MF C14H17ClN2O.HClMW 301.21
Purity:
99%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
PNU 282987 hydrochloride is an α7 nicotinic acetylcholine receptor (nAChR) agonist with Ki (α7 nAChR) and EC50 (α7-5HT3 chimera) values of 27 nm and 154 nM, respectively. PNU 282987 hydrochloride | | axonmedchem |