产品说明
生化/生理作用
VU0469650 is a brain-penetrant, potent and selective metabotropic glutamate receptor 1 (mGlu1) negative allosteric modulator (NAM). VU0469650 selectively inhibits glu-induced Ca2+ influx in human mGluR1-expressing HEK 293A (EC50 = 99 nM with [Glu] = EC20 for 1.9 min, then EC100 for 1.7 min; inactive against cells expressing human mGlu2-8 at 10 μM) with no affinity toward a panel of 68 clinically relevant GPCRs, ion channels, kinases, and transporters. Prior administration of VU0469650 in mice in vivo (60 mg/kg i.p.) modulates the antipsychotic activity of M4 muscarinic receptor PAM VU0467154 and that of the M1/M4 agonist xanomeline.
基本信息
经验(实验)分子式 | C22H28N4O · HCl |
分子量 | 400.94 |
产品性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | powder |
旋光性 | [α]/D -41 to -51°, c = 1 in methanol |
颜色 | white to beige |
溶解性 | DMSO: 2 mg/mL, clear (warmed) |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich