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BI-749327

CAS No. : 2361241-23-6

產(chǎn)品活性：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.

研究領(lǐng)域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶點(diǎn)：TRP Channel

In Vitro: 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: 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.).

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