| 产品描述： | 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 |
| 靶点： |
IC50: 13 nM (mouse TRPC6), 19 nM (human TRPC6), 15 nM (guinea pig TRPC6);TRP/TRPVChannel |
| 体外研究： |
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. |
| 体内研究： |
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. BI-749327 has long terminal half-life (t1/2 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: t1/2 8.5-13.5 hours |
| 参考文献： |
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. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.26 ml |
11.301 ml |
22.602 ml |
| 5 mM |
0.452 ml |
2.26 ml |
4.52 ml |
| 10 mM |
0.226 ml |
1.13 ml |
2.26 ml |
| 50 mM |
0.045 ml |
0.226 ml |
0.452 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京