盐酸瓦地那非三水合物 T4097

Product Introduction
Bioactivity


英文名: Vardenafil hydrochloride trihydrate

描述: Vardenafil hydrochloride trihydrate (BAY38-9456) 是一种新型 PDE 抑制剂，对 PDE5 和 PDE1 的 IC50 分别为 0.7 和 180 nM。

体外活性: Vardenafil specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM (6.6 nM). Vardenafil significantly enhances the SNP-induced relaxation of human trabecular smooth muscle at 3 nM (10 nM). Vardenafil also significantly potentiates both ACh-induced and transmural electrical stimulation-induced relaxation of trabecular smooth muscle. Vardenafil (100 mM) increases cyclic GMP levels in rat hippocampal slices. Vardenafil, tadalafil, and Sildenafil each competitively inhibit cGMP hydrolysis by phosphodiesterase-5 (PDE5), thereby fostering cGMP accumulation and relaxation of vascular smooth muscle.

体内活性: Vardenafil dose-dependently potentiates erectile responses to intravenously administered sodium nitroprusside in rabbit. Vardenafil (3 mg/kg, p.o.) results in an improved object discrimination performance in rats. Vardenafil (30 mg/L, p.o.) increases both iNOS and proliferating cell nuclear antigen expression (SM cell replication) in rats, with normalization of the dynamic infusion cavernosometry drop rate and SM/collagen ratio. Vardenafil induces powerful preconditioning-like cardioprotective effect against ischemia/reperfusion injury through the opening of mitochondrial K(ATP) channels in the heart of rabbit. Vardenafil protects the ischemic myocardium against reperfusion injury through a mechanism dependent on mitochondrial K(ATP) channel opening.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 93 mg/mL (160.6 mM)
H2O : 10 mg/mL (17.27 mM)
Ethanol : 16 mg/mL (27.6 mM)


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相关产品: OPC18750 HCl | Isopedicin | GSK356278 | Thioquinapiperifil dihydrochloride | PF-00489791 | PDE5-IN-2 | GEBR-7b | Pumafentrine | Isoprenaline hydrochloride | PDE4B-IN-2

相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | Approved Drug Library | Bioactive Lipid Compound Library | Inhibitor Library | EMA Approved Drug Library | Metabolism Compound Library | Endocrinology-Hormone Compound Library | NO PAINS Compound Library

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