VU0810464
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- CAS号:
- 2126040-21-7
- 英文名:
- VU0810464
- 英文别名:
- VU0810464;2-(3-Chloro-4-fluorophenyl)-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)acetamide;Benzeneacetamide, 3-chloro-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)-4-fluoro-;cells,KcsA,VU-0810464,Potassium Channel,neuronal GIRK,HPC,VU0810464,VU 0810464,SAN,inhibit,Inhibitor
- 中文名:
- VU0810464
- 中文别名:
- 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
- CBNumber:
- CB65839814
- 分子式:
- C18H21ClFN3O
- 分子量:
- 349.83
- MOL File:
- 2126040-21-7.mol
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VU0810464化学性质
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沸点:
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549.1±50.0 °C(Predicted)
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密度:
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1.31±0.1 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO: ≥ 250 mg/mL (714.63 mM)
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酸度系数(pKa):
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13.35±0.70(Predicted)
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VU0810464性质、用途与生产工艺
VU0810464 是有效的，选择性的非尿素蛋白门控的内向整流钾通道 (GIRK, Kir3) 激活剂。 VU0810464 对神经元 GIRK1/2 (EC50=165 nM) 和 GIRK1/4 (EC50=720 nM) 神经通道具有纳摩尔效价，并且具有脑部渗透性。
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.
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Animal Model:
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Male C57BL/6J mice, Kcnj3
−/−
siblings female and male C57BL/6J mice
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Dosage:
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10 mg/kg; 30mg/kg
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Administration:
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Intraperitoneal injection
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Result:
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Reduced stress‐induced hyperthermia (SIH), a physiological test of
anxiolytic efficacy in wild mice, but had no impact in and Kcnj3 (Girk1)
−/−
mice.
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VU0810464
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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-127106 | VU0810464 | | 1 mg | 1120元 |
| 2024/04/30 | HY-127106 | VU0810464
VU0810464 | 2126040-21-7 | 5mg | 2800元 |
2126040-21-7, VU0810464 相关搜索:
- 合成有机化合物配体
- 2-(3-氯-4-氟苯基)-N-(1-环己基-3-甲基-1H-吡唑-5-基)乙酰胺
- 化合物VU0810464
- 2126040-21-7
- cells,KcsA,VU-0810464,Potassium Channel,neuronal GIRK,HPC,VU0810464,VU 0810464,SAN,inhibit,Inhibitor
- 2-(3-Chloro-4-fluorophenyl)-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)acetamide
- Benzeneacetamide, 3-chloro-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)-4-fluoro-
- VU0810464