Human PDE5A1 (GenBank Accession No. NM_001083), full length, with N-terminal GST-tag, MW=126 kDa, expressed in a Baculovirus infected Sf9 cell expression system.

O76074

PDE5A, phosphodiesterase 5A

≥ 3100 pmol/min/µg

One unit is defined as the amount of enzyme that will convert 1 pmole of 3', 5'-cGMP to 5'-GMP per minute at 37°C.

Assayed using BPS's PDE5A kit, Cat. # 60350. Assay conditions: 10 mM Tris-HCl, pH 7.4, 10 mM MgCl₂, 0.1 mg/ml BSA, 0.05% Tween-20, 200 µM cGMP, 2.5 kU 5'-nucleotidase, and serial dilutions of PDE5A1 at 37°C for 20 min. Quantified by 5'- nucleotidase cleaving the 5' -GMP product and releasing the phosphate group which is detected by Malachite Green Reagent.

40mM Tris pH 8.0, 110mM NaCl, 2.2mM KCl, 0.04% Tween-20, 20% glycerol, 3mM DTT

Aqueous buffer solution

>6 months at -80°C.

Useful for the study of enzyme kinetics, screening inhibitors, and selectivity profiling.

1. Filippi,S. et al., Endocrinology 148 (3), 1019-1029 (2007).
2. Bruder,S. et al., J. Biol. Chem. 281 (29), 19969-19976 (2006).

Application Reference(s):
1. Discovery of a Novel Series of Pyrazolo[1,5-a]pyrimidine-Based Phosphodiesterase 2A Inhibitors Structurally Different from N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915), for the Treatment of Cognitive Disorders (2017)
2. Novel N-hydroxybenzamides incorporating 2-oxoindoline with unexpected potent histone deacetylase inhibitory effects and antitumor cytotoxicity. (2017)
3. Design and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders (2017)
4. Discovery of Selective Phosphodiesterase 1 Inhibitors with Memory Enhancing Properties (2017)
5. Identification and characterization of a potent and biologically-active PDE4/7 inhibitor via fission yeast-based assays (2017)
6. Characterization of the binding properties of T-773 as a PET radioligand for phosphodiesterase 10A (2015)
7. Active Site Coupling in PDE:PKA Complexes Promotes Resetting of Mammalian cAMP Signaling (2014)
8. Genetic deletion and pharmacological inhibition of phosphodiesterase 10A protects mice from diet-induced obesity and insulin resistance (2014)
9. A yeast-based chemical screen identifies a PDE inhibitor that elevates steroidogenesis in mouse Leydig cells via PDE8 and PDE4 inhibition (2013)
10. Analysis of substrate specificity and kinetics of cyclic nucleotide phosphodiesterases with N'-methylanthraniloyl-substituted purine and pyrimidine 3',5'-cyclic nucleotides by fluorescence spectrometry (2013)
11. The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey (2013)

Avoid freeze/thaw cycles.

PDE

Recombinant Protein