Gisadenafil besylate (UK 369003-26) is a specific, orally activephosphodiesterase5 (PDE5)inhibitor with anIC₅₀of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP)^[1].

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. TheIC₅₀of Gisadenafil for PDE5A is 3.6 nM. In contrast, theIC₅₀of Gisadenafil for PDE1A is 9.1 μM, an approximately 2500-fold difference in specificity^[1].

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^[1].

677.79

Solid

C₂₉H₃₉N₇O₈S₂

334827-98-4

吉沙那非苯磺酸盐

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

DMSO : 100 mg/mL(147.54 mM;Need ultrasonic)

H₂O : 3.33 mg/mL(4.91 mM;ultrasonic and warming and heat to 60℃)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。