BI-749327
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。 |
BI-749327 用途与合成方法
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 |
BI-749327 价格(试剂级)
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024-11-08 | HY-111925 | 1 mg | 1244 | ||
2024-11-08 | HY-111925 | BI-749327 | 2361241-23-6 | 5mg | 3500 |