BI-749327
| 中文名称 | BI-749327 |
|---|---|
| 中文同义词 | 化合物BI-749327 |
| 英文名称 | BI-749327 |
| 英文同义词 | BI-749327;Methanone, [4-(6-amino-3-pyridazinyl)-1-piperidinyl][4-[4-(trifluoromethyl)phenoxy]phenyl]-;BI749327,Inhibitor,BI-749327,inhibit,Transient receptor potential channels,BI 749327,TRP Channel;(4-(6-aminopyridazin-3-yl)piperidin-1-yl)(4-(4-(trifluoromethyl)phenoxy)phenyl)methanone |
| CAS号 | 2361241-23-6 |
| 分子式 | C23H21F3N4O2 |
| 分子量 | 442.43 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 2361241-23-6.mol |
| 结构式 |  |
BI-749327 性质
| 沸点 | 637.5±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.334±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C |
| 溶解度 | 溶于 DMSO (25 mg/ml) |
| 形态 | 固体 |
| 酸度系数(pKa) | 5.26±0.10(Predicted) |
| 颜色 | 白色 |
| 稳定性 | 自购买之日起 2 年内保持稳定。 DMSO 溶液可在 -20°C 下保存长达 2 个月。 |
IC50: 13 nM (mouse TRPC6), 19 nM (human TRPC6), 15 nM (guinea pig TRPC6)
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 has long terminal half-life (t
1/2
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: | t 1/2 8.5-13.5 hours |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-111925 | BI-749327 | 1 mg | 1244元 | |
| 2024/04/30 | HY-111925 | BI-749327 BI-749327 | 2361241-23-6 | 5mg | 3500元 |