BI-749327
|
|
|
- CAS号:
- 2361241-23-6
- 英文名:
- BI-749327
- 英文别名:
- BI-749327;(4-(6-aminopyridazin-3-yl)piperidin-1-yl)(4-(4-(trifluoromethyl)phenoxy)phenyl)methanone;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
- 中文名:
- BI-749327
- 中文别名:
- 化合物BI-749327
- CBNumber:
- CB95419686
- 分子式:
- C23H21F3N4O2
- 分子量:
- 442.43
- MOL File:
- 2361241-23-6.mol
|
|
|
BI-749327化学性质
-
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:
-
Soluble in DMSO (25 mg/ml)
-
|
-
形态:
-
solid
-
|
-
酸度系数(pKa):
-
5.26±0.10(Predicted)
-
|
-
颜色:
-
White
-
|
-
稳定性:
-
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
-
|
BI-749327性质、用途与生产工艺
BI-749327 是一种高效、高选择性、有口服生物活性的 TRPC6 拮抗剂，对小鼠、人、豚鼠 TRPC6 作用的 IC50 值分别为 13 nM、19 nM 和 15 nM。BI-749327 对小鼠 TRPC6 的选择性是 TRPC3 的 85 倍， 是 TRPC7 的 42 倍。
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
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
2361241-23-6, BI-749327 相关搜索:
- 化合物BI-749327
- 2361241-23-6
- (4-(6-aminopyridazin-3-yl)piperidin-1-yl)(4-(4-(trifluoromethyl)phenoxy)phenyl)methanone
- BI749327,Inhibitor,BI-749327,inhibit,Transient receptor potential channels,BI 749327,TRP Channel
- Methanone, [4-(6-amino-3-pyridazinyl)-1-piperidinyl][4-[4-(trifluoromethyl)phenoxy]phenyl]-
- BI-749327