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编 号:F281760
分子式:C23H33ClN6O4S
分子量:525.06
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10mM*1mL in DMSO
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100mg
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200mg
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生物活性:
Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes-.

体内研究:
Vardenafil hydrochloride (IV;0.03 mg/kg) 对海绵体神经损伤大鼠具有促进作用。Vardenafil hydrochloride (IV;0.17 mg/kg,每天一次;7 天) 保护肝脏对抗 Con A 诱导的肝炎,并降低肝组织中 NF-。Vardenafil hydrochloride (口服;10 mg/kg,每日一次;25 周) 防止组织 cGMP 水平的降低和 ZDF 心脏中 3-NT 生成的增加。Animal Model:Male rat (9-week-old) underwent surgery for laparotomy or bilateral cavernous nerve (CN) crush injury
Dosage:0.03 mg/kg
Administration:Intravenous injection
Result:Restored normal erectile responses with a combind administration of BAY 60-4552 (0.03, 0.3 mg/kg).
Animal Model:Liver injury induced by Con A in male Swiss albino mice (20 ± 2 g)
Dosage:0.17 mg/kg
Administration:Intravenous injection; once daily, for 7 days; as a pretreatment
Result:Reduced the levels of serum transaminases and alleviated Con A-induced hepatitis.
Animal Model:Male 7-week-old Zucker diabetic fatty (ZDF) rats (preserved ejection fraction, HFpEF)
Dosage:10 mg/kg
Administration:Oral gavage; once daily, for 25 weeks
Result:Improved myofilament function in diabetic rat hearts.

体外研究:
Vardenafil hydrochloride 特异性抑制 PDE5 对 cGMP 的水解,IC50 为 0.7 nM。Vardenafil hydrochloride 增加阴茎海绵体组织中的细胞内 cGMP 水平,从而导致身体鼻窦扩张和血流量增加。
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