VU0810464
| 中文名称 | VU0810464 |
|---|---|
| 中文同义词 | 化合物VU0810464;2-(3-氯-4-氟苯基)-N-(1-环己基-3-甲基-1H-吡唑-5-基)乙酰胺 |
| 英文名称 | VU0810464 |
| 英文同义词 | VU0810464;Benzeneacetamide, 3-chloro-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)-4-fluoro-;2-(3-Chloro-4-fluorophenyl)-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)acetamide;cells,KcsA,VU-0810464,Potassium Channel,neuronal GIRK,HPC,VU0810464,VU 0810464,SAN,inhibit,Inhibitor |
| CAS号 | 2126040-21-7 |
| 分子式 | C18H21ClFN3O |
| 分子量 | 349.83 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 2126040-21-7.mol |
| 结构式 |  |
VU0810464 性质
| 沸点 | 549.1±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.31±0.1 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：≥ 250 mg/mL（714.63 mM） |
| 酸度系数(pKa) | 13.35±0.70(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
EC50: 165 nM (GIRK 1/2); 720 nM (GIRK1/4 )
VU0810464 (0, 0.1, 0.3, 1, 3, 10, 30 μM) produces a concentration‐dependent response curves of currents in SAN and HPC cells, in addition, VU0810464 is 9‐fold higher potency for Kir3 channel activation in neurons as compared to SAN cells.
VU0810464 (intraperitoneal injection; 30 mg/kg, 10 mg/kg; 30mg/kg; pre-treated 30 mins) produces a dose-dependent reduction of SIH response in Male C57BL/6J mice. To test if VU0810464 plays it role through Kir3 channel activation, VU0810464 (10 mg/kg) suppresses the SIH response in wild‐ type mice, but has no impact on Kcnj3 −/− mice. VU0810464 (intraperitoneal injection ; 30 mg/kg; 15, 30, 45, or 60 min post‐injection) displays a favourable distribution to the brain (K p,uu = 0.83), has a improvement over ML297 (K p,uu = 0.32). Clearance of VU0810464 is rapid,brain and plasma half-lives is 20 min in a PK study.
| Animal Model: | Male C57BL/6J mice, Kcnj3 −/− siblings female and male C57BL/6J mice |
| Dosage: | 10 mg/kg; 30mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | Reduced stress‐induced hyperthermia (SIH), a physiological test of anxiolytic efficacy in wild mice, but had no impact in and Kcnj3 (Girk1) −/− mice. |
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-127106 | VU0810464 | 1 mg | 1120元 | |
| 2024/04/30 | HY-127106 | VU0810464 VU0810464 | 2126040-21-7 | 5mg | 2800元 |