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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-VA-012
VA-012

Chemical Structure : VA-012

CAS No.: 885898-58-8

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VA-012 (VA012)

货号: PC-62010Not For Human Use, Lab Use Only.

VA-012 is a potent, selective 5-HT2C receptor positive allosteric modulator (PAM) that exhibits dose-dependent potentiation of 5-HT efficacy with EC50 of 16 nM.

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

    生物&药学活性

    VA-012 is a potent, selective 5-HT2C receptor positive allosteric modulator (PAM) that exhibits dose-dependent potentiation of 5-HT efficacy with EC50 of 16 nM.
    VA-012 shows no significant off-target activities, and low binding competition with serotonin or other orthosteric ligands.
    VA-012 increases the anorectic effect combined with the SSRI sertraline.
    VA-012 reduces food intake and body weight gain without causing CNS-related malaise.

    物理化学性质&存储条件

    分子量 313.4
    分子式 C21H19N3
    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

    1-(Phenylmethyl)-N-3-pyridinyl-1H-indole-3-methanamine

    参考文献

    1. García Cárceles J, et al. J Med Chem. 2017 Nov 8. doi: 10.1021/acs.jmedchem.7b00994.

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