UK-369003

Research use only, not for human use.

UK-369003 (Gisadenafil besylate) is a novel, potent, selective, orally bioavailable PDE5 inhibitor with IC50 of 1.23 nM.

UK-369003 (Gisadenafil besylate) is a novel, potent, selective, orally bioavailable PDE5 inhibitor with IC50 of 1.23 nM, displays 117-fold selectivity over PDE6; demonstrates efficacy in patients with lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH).COPD Phase 2 Discontinued.

Since some PDE5 inhibitors can also interact with PDE1 isotypes found within the cerebral vasculature, the specificity of Gisadenafil for PDE5 is confirmed. This is directly tested with recombinant PDE5A and PDE1A overexpressed in COS-7 cells. The IC50 of Gisadenafil for PDE5A is 3.6 nM. In contrast, the IC50 of Gisadenafil for PDE1A is 9.1 μM, an approximately 2500-fold difference in specificity.

Gisadenafil (2 mg/kg; intraperitoneal injection; for 2 hours; male Tat-transgenic mice) treatment largely restores the normal increase in cortical flow following hypercapnia in Tat-tg mice (17.5% above baseline). Gisadenafil also restores the dilation of small (<25 μm) arterioles following hypercapnia, although it fails to restore full dilation of larger (>25 μm) vessels. Animal Model:Male Tat-transgenic (Tat-tg) mice (8 weeks old) exposed to hypercapnia Dosage:2 mg/kg Administration:Intraperitoneal injection; for 2 hours Result:Largely restored the normal increase in cortical flow following hypercapnia in Tat-tg mice (17.5% above baseline). Also restored the dilation of small (<25 μm) arterioles following hypercapnia.

Gisadenafil besylate

Angiogenesis

PDE

PDE

Inflammation/Immunology

COPD

334827-98-4

677.79

C23H33N7O5S.C6H6O3S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (147.54 mM)

CCC1=C2C(=NN1CCOC)C(=O)NC(=N2)C3=C(N=CC(=C3)S(=O)(=O)N4CCN(CC4)CC)OCC.C1=CC=C(C=C1)S(=O)(=O)O

5-[2-Ethoxy-5-[(4-ethyl-1-piperazinyl)sulfonyl]-3-pyridinyl]-3-ethyl-2,6-dihydro-2-(2-methoxyethyl)-7H-pyrazolo[4,3-d]pyrimidin-7-one benzenesulfonate

(-20℃)

With Ice Pack

≥ 2 years