2361241-23-6
2361241-23-6 結構式
基本信息
Methanone, [4-(6-amino-3-pyridazinyl)-1-piperidinyl][4-[4-(trifluoromethyl)phenoxy]phenyl]-
物理化學性質
常見問題列表
IC50: 13 nM (mouse TRPC6), 19 nM (human TRPC6), 15 nM (guinea pig TRPC6)
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 (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 (t
1/2
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: | t 1/2 8.5-13.5 hours |