VU0360223
货号：
11995-1mg 基本售价：
350.0 元 规格：
1 mg
产品信息
概述| 货号 | 11995-1mg |
| 描述 | Glutamate, the major excitatory neurotransmitter in the central nervous system, 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. VU0360223 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.1 A 10 μM concentration of VU0360223 results in a near complete blockade of the glutamate response in cortical astrocytes.1 A 30 mg/kg dose of VU0360223 in mice yields potent inhibition in a marble burying model of anxiety and is efficacious in an operant sensation seeking model of addiction.1 |
| 别名 | CAY10651; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Lindsley, C.W.,Bates, B.S.,Menon, U.N., et al. (3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu5: Discovery of a new tool compound with activity in the OSS mouse model of addiction. ACS Chem.Neurosci. 2, 471-482 (2011).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 268.3 |
| 分子式 | C15H9FN2S |
| CAS号 | 1274859-33-4 |
| 稳定性 | ≥ 2 years |
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