PDE5-IN-2

Modify Date: 2024-01-10 12:19:38

PDE5-IN-2 Structure
PDE5-IN-2 structure
Common Name PDE5-IN-2
CAS Number 2244517-61-9 Molecular Weight 491.52
Density N/A Boiling Point N/A
Molecular Formula C25H21N3O6S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PDE5-IN-2


PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC50 of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC50s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity[1].

 Names

Name PDE5-IN-2

 PDE5-IN-2 Biological Activity

Description PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC50 of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC50s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity[1].
Related Catalog
Target

PDE5A1:0.31 nM (IC50)

PDE6C:1.2 nM (IC50)

PDE4D2:43 nM (IC50)

PDE10A:46 nM (IC50)

PDE2A:106 nM (IC50)

In Vitro PDE5-IN-2 (Compound 3) has at least 1000-fold selectivity over PDE1B, PDE3A, PDE7A1, PDE8A1, and PDE9A2 (IC50s, >32 000 nM)[1].
In Vivo PDE5-IN-2 (1.25 mg/kg, p.o.) shows anti-pulmonary arterial hypertension activity, decreases mean pulmonary artery pressure in rats[1].
References

[1]. Wu D, et al. Optimization of Chromeno[2,3- c]pyrrol-9(2 H)-ones as Highly Potent, Selective, and Orally Bioavailable PDE5 Inhibitors: Structure-Activity Relationship, X-ray Crystal Structure, and Pharmacodynamic Effect on Pulmonary Arterial Hypertension. J Med Chem. 2018 Sep 27;61(18):8468-8473.

 Chemical & Physical Properties

Molecular Formula C25H21N3O6S
Molecular Weight 491.52