BYK 191023 dihydrochloride

BYK 191023 dihydrochlorideCAS号: 1216722-25-6分子式: C14H14N4O • 2HCl分子量: 327.21描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述

BYK191023 is a selective inhibitor of the inducible nitric-oxide synthase (NOS).

纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
BYK 191023 2HCl
可溶性/溶解性
Soluble in H2O
生物活性
靶点
iNOS
In vitro(体外研究)
BYK191023 showed half-maximal inhibition of crudely purified human inducible, neuronal, and endothelial NO synthases at 86 nM, 17 μM, and 162 μM, respectively. The ihibition of inducible NO synthase was competitive with L-arginine, pointing to an interaction of BYK191023 with the catalytic center of the enzyme. BYK191023 did not show any toxicity in various rodent and human cell lines up to high micromolar concentrations.
In vivo(体内研究)
Authors tested the in vivo potency of BYK191023 in rat models of lipopolysaccharide-induced systemic inflammation. Delayed administration of BYK191023 suppressed the LPS-induced increase in plasma nitrate/nitrite (NOx) levels with an ED50 of 14.9 μmol/kg/h dose-dependently. In a systemic hypotension model following high-dose lipopolysaccharide challenge, curative administration of BYK191023 at a dose that inhibited 83% of the Nox increase completely prevented the gradual decrease in mean arterial blood pressure observed in control animals.

分子结构图

BYK 191023 dihydrochloride