VU 0361737
规格
Cas Number | 1161205-04-4(DMSO) |
规格或纯度 | Moligand™, 10mM in DMSO |
级别 | Moligand™ |
包装 | 1ml |
产品信息
品牌 | 阿拉丁 |
浓度 | 10mM in DMSO |
Action Type | 变构调节剂 |
Mechanism Of Action | mGlu 4 受体的异构调节剂 |
溶解性 | Solubility (25°C) In vitro DMSO: 58 mg/mL (199.49 mM); |
简短描述 | mGluR4 Selective Agonists |
英文简短描述 | mGluR4 Selective Agonists |
过滤标签 | Compound libraries |
储存温度 | -80℃储存 |
运输条件 | 超低温冰袋运输 |
生化和生理学机理 | VU 0361737 是一种针对 mGlu4 受体的选择性正性异位调节剂(PAM),对人类和大鼠受体的 EC50 分别为 240 nM 和 110 nM,对 mGlu5 和 mGlu8 受体的活性较弱,对 mGlu1、mGlu2、mGlu3、mGlu6 和 mGlu7 受体无活性,可渗透至中枢神经系统。 |
描述 |
VU 0361737是一种选择性mGlu4受体正变构调节剂 (PAM), 作用于人类和大鼠受体, EC50分别为240 nM和110 nM, 对mGlu5和mGlu8受体具有微弱的作用活性,a selective positive allosteric modulator at mGluR-4 |
英文描述 |
Information VU 0361737 is a selective positive allosteric modulator (PAM) formGlu4receptor withEC50of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 VU0361737 is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. In vivo VU0361737 shows high in vivo CL in rat, a short half-life (T1/2 20 min), and demonstrates significant brain exposure (brain-to-plasma ratio of 4.1). cell lines: Concentrations: Incubation Time: Powder Purity:≥100% |