VU0810464
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) |
VU0810464 用途与合成方法
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. |
VU0810464 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-01-25 | HY-127106 | 1 mg | 1400 | ||
| 2024-01-25 | HY-127106 | VU0810464 | 2126040-21-7 | 5mg | 3500 |
