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CTEP (RO4956371),mGlu5 受体别构拮抗剂

CTEP (RO4956371) （订货以英文为准）

编号：C126237
CAS号：871362-31-1
分子式：C19H13CLF3N3O
分子量：391.77
货号 品牌 包装 目录价 您的价格 库存 数量 购买
C126237-10mg 阿拉丁 10mg ¥1231.90
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C126237-50mg 阿拉丁 50mg ¥4741.90
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C126237-5mg 阿拉丁 5mg ¥770.90
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C126237-1mg 阿拉丁 1mg ¥404.90
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C126237-100mg 阿拉丁 100mg ¥6681.90
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C126237-25mg 阿拉丁 25mg ¥2761.90
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产品名称 CTEP (RO4956371)
中文名称 CTEP (RO4956371),mGlu5 受体别构拮抗剂
CAS号 871362-31-1
MDL编码 MFCD22665726
分子式（M.F.） C19H13CLF3N3O
分子量（M.W.） 391.77
储存条件 避光;-20°C储存;干燥
溶解性DMSO 78 mg/mL Water <1 mg/mL Ethanol 10 mg/mL
存贮条件储存温度-20°C
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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