| Bioactivity | 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[1]. | ||||||||||||
| Target | IC50: 13 nM (mouse TRPC6), 19 nM (human TRPC6), 15 nM (guinea pig TRPC6) | ||||||||||||
| Invitro | 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[1]. | ||||||||||||
| 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[1].BI-749327 dose dependently reduces renal fibrosis and associated gene expression in mice with unilateral ureteral obstruction[1].BI-749327 has long terminal half-life (t1/2 8.5-13.5 hours) for mice (3-30 mg/kg; p.o.)[1]. Animal Model: | ||||||||||||
| Name | BI-749327 | ||||||||||||
| CAS | 2361241-23-6 | ||||||||||||
| Formula | C23H21F3N4O2 | ||||||||||||
| Molar Mass | 442.43 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Lin B L, et al. In vivo selective inhibition of TRPC6 by antagonist BI 749327 ameliorates fibrosis and dysfunction in cardiac and renal disease. Proc Natl Acad Sci U S A. 2019 May 14;116(20):10156-10161. |
BI-749327
CAS: 2361241-23-6 F: C23H21F3N4O2 W: 442.43
BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM f
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