BI-749327是高选择性、口服有效的TRPC6拮抗剂，对小鼠、人、豚鼠 TRPC6 作用的IC50值分别为 13 nM、19 nM 和 15 nM。BI-749327对小鼠 TRPC6 选择性比 TRPC3 高出 85 倍， 比TRPC7高出42 倍。

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).

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.

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.

2361241-23-6

C23H21F3N4O2

442.43

DMSO:31.25 mg/mL (70.63 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years