VU0810464
- CAS号:2126040-21-7
- 英文名:VU0810464
- 中文名:VU0810464
- CBNumber:CB65839814
- 分子式:C18H21ClFN3O
- 分子量:349.83
- MOL File:2126040-21-7.mol
- 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 :DMSO: ≥ 250 mg/mL (714.63 mM)
- 酸度系数(pKa) :13.35±0.70(Predicted)
- 形态 :Solid
- 颜色 :White to off-white
VU0810464性质、用途与生产工艺
- 生物活性 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。
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靶点
EC50: 165 nM (GIRK 1/2); 720 nM (GIRK1/4 )
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体外研究
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.
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体内研究
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.
- 更新日期：2024/11/08
- 产品编号：HY-127106
- 产品名称：VU0810464
- CAS编号：
- 包装：1 mg
- 价格：1120元
- 更新日期：2024/11/08
- 产品编号：HY-127106
- 产品名称：VU0810464 VU0810464
- CAS编号：2126040-21-7
- 包装：5mg
- 价格：2800元
- 公司名称：TargetMol Chemicals Inc.
- 联系电话：+1-781-999-5354 +1-00000000000
- 电子邮件：marketing@targetmol.com
- 国家：美国
- 产品数：32161
- 优势度：58
- 公司名称：Aladdin Scientific
- 联系电话：+1-+1(833)-552-7181
- 电子邮件：sales@aladdinsci.com
- 国家：美国
- 产品数：57505
- 优势度：58
- 公司名称：TargetMol Chemicals Inc.
- 联系电话：
- 电子邮件：support@targetmol.com
- 国家：美国
- 产品数：38631
- 优势度：58
- 公司名称：MedChemExpress
- 联系电话：--
- 电子邮件：sales@medchemexpress.com
- 国家：美国
- 产品数：6398
- 优势度：58
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