VU0483605
货号：
16941-1mg 基本售价：
490.0 元 规格：
1 mg
产品信息
概述| 货号 | 16941-1mg |
| 描述 | Glutamate, the major excitatory neurotransmitter in the CNS, activates eight known subtypes of metabotropic glutamate receptors (mGluRs). Highly selective modulators designed to act at allosteric sites on certain mGluR subtypes are being developed to preferentially regulate subtype-specific, glutamate-induced receptor activation.1 VU0483605 is a selective positive allosteric modulator (PAM) of mGluR1, displaying EC50 values of 0.39 and 0.36 μM at human and rat receptors, respectively, and no activity as a mGlu4 PAM (EC50 >10 μM).2 It has been shown to potentiate a response to glutamate in wild-type cell lines stably expressing mGlu1 and to partially restore the reduction in glutamate-mediated calcium signaling in a mutant cell model of schizophrenia.2 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Sheffler, D.J., and Conn, P.J. Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells. Neuropharmacology 55(4), 419-427 (2008).
2.Cho, H.P.,Garcia-Barrantes, P.M.,Brogan, J.T., et al. Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics. ACS Chemical Biology 9(10), 2234-2246 (2014).
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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 | 446.7 |
| 分子式 | C20H10Cl3N3O3 |
| CAS号 | 1623101-11-0 |
| 稳定性 | ≥ 2 years |
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