215258-13-2
| 中文名称 | 215258-13-2 |
|---|---|
| 中文同义词 | 化合物 FR167344 free base |
| 英文名称 | FR167344 free base |
| 英文同义词 | FR167344 free base;Benzamide, 4-[(1E)-3-[[2-[[3-[[(3-bromo-2-methylimidazo[1,2-a]pyridin-8-yl)oxy]methyl]-2,4-dichlorophenyl]methylamino]-2-oxoethyl]amino]-3-oxo-1-propen-1-yl]-N,N-dimethyl- |
| CAS号 | 215258-13-2 |
| 分子式 | C30H28BrCl2N5O4 |
| 分子量 | 673.39 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 215258-13-2.mol |
| 结构式 |  |
215258-13-2 性质
| 密度 | 1.43±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 12.58±0.46(Predicted) |
IC50: 65 nM (Bradykinin receptor B2)
In competitive experiments using membranes prepared from Chinese hamster ovary cells expressing the bradykinin receptor subtypes, FR167344 shows a high affinity binding to the B2 receptor with IC 50 values of 65 nM, and no binding affinity for the B1 receptor. FR167344 inhibits the B2 receptor-mediated phosphatidylinositol (PI) hydrolysis and produces a concentration-dependent rightward shift in the dose-response curve to bradykinin. This shift is accompanied by a progressive reduction of maximal response. Estimated pA2 values for the antagonism of bradykinin induced PI hydrolysis by FR167344 is 8.0. FR167344 shows no stimulatory effects on PI hydrolysis.
Oral administration of FR167344 inhibits carrageenin-induced paw oedema in rats with an ID 50 of 2.7 mg/kg at 2h after carrageenin injection. Oral administration of FR167344 inhibits kaolin-induced writhing in mice with an ID 50 of 2.8 mg/kg in 10 min writhing and 4.2 mg/kg in 15 min writhing. Oral administration of FR167344 inhibits caerulein-induced pancreatic oedema with an ID 50 of 13.8 mg/kg as well as increases in amylase and lipase of blood samples with ID 50 of 10.3 and 7.4 mg/kg, respectively, in rats.