中文名称

CAY10651 (10 mg)

英文名字

CAY10651, 3-fluoro-5-(2-methylbenzo(d)thiazol-5-yl)-benzonitrile

供应商

Cayman

产品货号

10820-10

产品报价

￥3360/10 mg

产品说明书

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购买方式

产品新闻

背景资料

Glutamate, the major excitatory neurotransmitter in the CNS, signals through both ionotropic and metabotropic glutamate receptors. Of the eight metabotropic glutamate receptors -mGlus) discovered thus far, development of inhibitors to mGlu5 has been given significant attention in preclinical models of disease, including pain, anxiety, gastresophageal reflux disease, Parkinson s associated dyskinesia, and fragile X syndrome, as well as in animal models of drug addiction. CAY10651 is a noncompetitive antagonist -negative allosteric modulator) of mGlu5 that demonstrates an IC50 value of 61 nM in a calcium mobilization assay and a Ki value of 477 nM in a radioligand binding assay. A 10 uM concentration of CAY10651 results in a near complete blockade of the glutamate response in cortical astrocytes. A 30 mg/kg dose of CAY10651 in mice yields potent inhibition in a marble burying model of anxiety and is efficacious in an operant sensation seeking model of addiction.

产品描述

A noncompetitive antagonist of mGlu5 -IC50 = 61 nM; Ki = 477 nM); 10 uM results in a near complete blockade of the glutamate response in cortical astrocytes; 30 mg/kg in mice yields potent inhibition in a marble burying model of anxiety and is efficacious in an operant sensation seeking model of addiction

产品形式

保存建议

-20

其他

Cayman Chemical

注意

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