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首页-小分子抑制剂&激动剂-GPCR-mGluR-VU0400195
VU0400195

Chemical Structure : VU0400195

CAS No.: 1309434-83-0

VU0400195 (ML182)

货号: PC-62957Not For Human Use, Lab Use Only.

VU0400195 (ML 182) is a potent, selective, brain penetrant and orally active positive allosteric modulator of mGluR4 with EC50 of 291 nM and 376 nM for human and rat mGluR4, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    VU0400195 (ML 182) is a potent, selective, brain penetrant and orally active positive allosteric modulator of mGluR4 with EC50 of 291 nM and 376 nM for human and rat mGluR4, respectively.
    VU0400195 shows no activity against mGlu1, 2, 3, and 8 and active against mGlu5 (PAM, EC50=1.7 uM), mGlu6 (PAM, EC50>10 uM) and mGlu7 (PAM, EC50=2.9 uM).
    VU0400195 reverses haloperidol-induced catalepsy, a preclinical rodent model of motor impairments associated with Parkinson’s disease.

    物理化学性质&存储条件

    分子量 393.827
    分子式 C21H16ClN3O3
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    N-[3-Chloro-4-[(3aR,4S,7R,7aS)-1,3,3a,4,7,7a-hexahydro-1,3-dioxo-4,7-methano-2H-isoindol-2-yl]phenyl]-2-pyridinecarboxamide

    参考文献

    1. Jones CK, et al. J Med Chem. 2011 Nov 10;54(21):7639-47.

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