Gisadenafil

Research use only, not for human use.

Gisadenafil is a selective inhibitor of phosphodiesterase 5 (PDE5) with an IC50 of 3.6 nM and prevents degradation of cGMP.

Gisadenafil is a selective inhibitor of phosphodiesterase 5 (PDE5) with an IC50 of 3.6 nM and prevents degradation of cGMP.(In Vitro):In COS-7 cells, the IC50 of Gisadenafil for PDE1A is 9.1 μM, an approximately 2500-fold difference in selectivity.(In Vivo):In male Tat-transgenic mice, Gisadenafil (2 mg/kg; i.p.) restores the dilation of small (<25 μm) arterioles following hypercapnia, although it fails to restore full dilation of larger (>25 μm) vessels. Gisadenafil largely restores the normal increase in cortical flow following hypercapnia in Tat-tg mice (17.5% above baseline).

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.

UK-369003

Angiogenesis

PDE

Estrogen Receptor/ERR| Human Endogenous Metabolite

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334826-98-1

519.62

C23H33N7O5S

>98% (HPLC)

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CCOc1ncc(cc1-c1nc2c(CC)n(CCOC)nc2c(=O)[nH]1)S(=O)(=O)N1CCN(CC)CC1

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(-20℃)

With Ice Pack

≥ 2 years