BI-749327 |
カタログ番号GC34489 |
BI-749327 は、マウス、ヒト、およびモルモットの TRPC6 に対してそれぞれ 13 nM、19 nM、および 15 nM の IC50 を持つ、強力で選択性の高い経口投与可能な TRPC6 アンタゴニストです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2361241-23-6
Sample solution is provided at 25 µL, 10mM.
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].
IC50: 13 nM (mouse TRPC6), 19 nM (human TRPC6), 15 nM (guinea pig TRPC6)[1]
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].
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].
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.
Average Rating: 5
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