PDE5-IN-2

Names

[ CAS No. ]:
2244517-61-9

[ Name ]:
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]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)

[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

Related Compounds