产品
编 号：F286606
分子式：C23H21F3N4O2
分子量：442.43
分子式：C23H21F3N4O2
分子量：442.43
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
4800
In-stock
1mg
1490
In-stock
5mg
4320
In-stock
10mg
6420
In-stock
50mg
0
In-stock
结构图
CAS No: 2361241-23-6
产品详情
生物活性：
BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7.
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 has long terminal half-life (t1/2 8.5-13.5 hours) for mice (3-30 mg/kg; p.o.).Animal Model:C57BL/6J mice
Dosage:30 mg/kg/day
Administration:Oral gavage
Result:Improved left heart function, reduced volume/mass ratio, and blunted expression of profibrotic genes and interstitial fibrosis in mice subjected to sustained pressure overload.
Animal Model:CD-1 mice
Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg
Administration:Oral administration
Result:t1/2 8.5-13.5 hours
体外研究：
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.
BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7.
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 has long terminal half-life (t1/2 8.5-13.5 hours) for mice (3-30 mg/kg; p.o.).Animal Model:C57BL/6J mice
Dosage:30 mg/kg/day
Administration:Oral gavage
Result:Improved left heart function, reduced volume/mass ratio, and blunted expression of profibrotic genes and interstitial fibrosis in mice subjected to sustained pressure overload.
Animal Model:CD-1 mice
Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg
Administration:Oral administration
Result:t1/2 8.5-13.5 hours
体外研究：
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.
产品资料
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