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产品介绍
产品介绍
产品信息
抗原名称
mouse TRPC6:13 nM (IC50), human TRPC6:19 nM (IC50), guinea pig TRPC6:15 nM (IC50)
商品描述
BI-749327 is a high selectivity and orally bioavailable antagonist of TRPC6 (IC50s: 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6).
分子量
442.43
纯度
98%
可溶性
DMSO:31.25 mg/mL (70.63 mM)
In vitro(体外研究)
BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7. BI-749327 suppresses NFAT activation in HEK293T cells expressing wild-type or gain-of-function TRPC6 mutants and blocks associated signaling and expression of prohypertrophic genes in isolated myocytes.
In vivo(体内研究)
BI-749327 (30 mg/kg/day; i.g.) improves left heart function, reduces volume/mass ratio, and blunts expression of profibrotic genes and interstitial fibrosis in mice subjected to sustained pressure overload. BI-749327 dose-dependently reduces renal fibrosis and associated gene expression in mice with unilateral ureteral obstruction. BI-749327 (3-30 mg/kg; p.o.) has a long terminal half-life (t1/2 8.5-13.5 hours) for mice.
背景
分子式
C23H21F3N4O2
CAS号
2361241-23-6
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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