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CTEP (RO4956371)
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
阿拉丁 | 生产商 | 上海 | 现货 |
货号 | CAS号 | 操作 |
---|---|---|
C126237-10mg | 871362-31-1 | 询价 |
C126237-1mg | 871362-31-1 | 询价 |
C126237-50mg | 871362-31-1 | 询价 |
C126237-5mg | 871362-31-1 | 询价 |
- 分子式 C19H13ClF3N3O
- 分子量391.77
属性
溶解性 |
|
存贮条件 | 储存温度-20°C |
描述
备注 | CTEP is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, shows >1000-fold selectivity over other mGlu receptors. |
生化机理 |
The metabotropic glutamate receptor 5 (mGlu5) is a glutamate-activated class C G protein-coupled receptor widely expressed in the central nervous system and clinically investigated as a drug target for a range of indications, including depression, Parkinson's disease, and fragile X syndrome. CTEP is a novel, potent, selective and orally bioavailable allosteric antagonist of the metabotropic glutamate receptor subtype mGluR5. CTEP binds mGlu5 with low nanomolar affinity and shows >1000-fold selectivity when tested against 103 targets, including all known mGlu receptors. In animal studies CTEP was found to have a high oral bioavailability and a long duration of action, lasting 18 hours after a single dose, giving it considerably improved properties over older mGluR5 antagonists such as MPEP and fenobam. |
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途