CS-2729
| 中文名称 | CS-2729 |
|---|---|
| 中文同义词 | 化合物 T13321;化合物VU6005649;VU 6005649,MGLU7和MGLU8受体的正变构调节剂 |
| 英文名称 | VU6005649 |
| 英文同义词 | VU6005649;VU-6005649;VU 6005649;VU6005649; VU-6005649; VU 6005649;CS-2729;Pyrazolo[1,5-a]pyrimidine, 3-(2,3-difluoro-4-methoxyphenyl)-2,5-dimethyl-7-(trifluoromethyl)-;Inhibitor,inhibit,VU6005649,mGluR,Metabotropic glutamate receptors,VU 6005649,VU-6005649 |
| CAS号 | 2137047-43-7 |
| 分子式 | C16H12F5N3O |
| 分子量 | 357.28 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 2137047-43-7.mol |
| 结构式 |  |
CS-2729 性质
| 密度 | 1.43±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | -1.73±0.30(Predicted) |
|
mGlu7 Receptor 0.65 μM (EC 50 ) |
mGlu8 Receptor 2.6 μM (EC 50 ) |
VU6005649 is a CNS penetrant mGlu 7/8 receptor agonist with EC 50 s of 0.65 μM and 2.6 μM for mGlu 7 receptor and mGlu 8 receptor, respectively. VU6005649 displays a terminal K p of 2.43 with total brain levels ~9× above the mGlu 7 positive allosteric modulator (PAM) in vitro EC 50 .
When VU6005649 (compound 9f) is dosed at 30 mg/kg IP in 10% Tween 80/H 2 O (0.75 mg/kg. s.c. amphetamine), no efficacy is observed in this assay. VU6005649 shows modest but significant pro-cognitive effects on associative learning in wild-type mice and the first example of efficacy of an mGlu 7/8 positive allosteric modulator (PAM) in this model.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-107982 | CS-2729 VU6005649 | 2137047-43-7 | 5mg | 900元 |
| 2024/01/25 | HY-107982 | CS-2729 VU6005649 | 2137047-43-7 | 10mM * 1mLin DMSO | 990元 |