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CTEP (RO4956371),mGlu5 受体别构拮抗剂

规格或纯度: 98%
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货号 (SKU) 包装规格 是否现货 价格 数量
C126237-1mg
1mg 现货 Stock Image
C126237-5mg
5mg 现货 Stock Image
C126237-10mg
10mg 现货 Stock Image
C126237-25mg
25mg 现货 Stock Image
C126237-50mg
50mg 现货 Stock Image
C126237-100mg
100mg 现货 Stock Image

基本描述

英文别名 CTEP|871362-31-1|2-chloro-4-((2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1H-imidazol-4-yl)ethynyl)pyridine|CTEP (RO4956371)|mGluR5 inhibitor|2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine|E3BWG5775S|CHEMBL3410223
规格或纯度 98%
英文名称 CTEP (RO4956371)
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 drμg 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.

储存温度 避光,-20°C储存,干燥
运输条件 超低温冰袋运输
产品介绍

用途:

它是一种新颖的,长效的,可口服的 mGlu5 受体别构拮抗剂,IC50 值为 2.2 nM,对其选择性是对其他 mGlu 受体的 1000 多倍。


名称和标识符

IUPAC Name 2-chloro-4-[2-[2,5-dimethyl-1-[4-(trifluoromethoxy)phenyl]imidazol-4-yl]ethynyl]pyridine
INCHI InChI=1S/C19H13ClF3N3O/c1-12-17(8-3-14-9-10-24-18(20)11-14)25-13(2)26(12)15-4-6-16(7-5-15)27-19(21,22)23/h4-7,9-11H,1-2H3
InChi Key GOHCTCOGYKAJLZ-UHFFFAOYSA-N
Canonical SMILES CC1=C(N=C(N1C2=CC=C(C=C2)OC(F)(F)F)C)C#CC3=CC(=NC=C3)Cl
Isomeric SMILES CC1=C(N=C(N1C2=CC=C(C=C2)OC(F)(F)F)C)C#CC3=CC(=NC=C3)Cl
关联CAS 871362-31-1
PubChem CID 11646823
MeSH Entry Terms 2-chloro-4-((2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1H-imidazol-4-yl)ethynyl)pyridine;CTEP cpd;RO 4956371;RO-4956371;RO4956371
分子量 391.77

化学和物理性质

溶解性 DMSO 78 mg/mL Water <1 mg/mL Ethanol 10 mg/mL
敏感性 对光线和湿度敏感

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