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首页-小分子抑制剂&激动剂-GPCR-Dopamine Receptor-GSK598809
GSK598809

Chemical Structure : GSK598809

CAS No.: 863680-45-9

GSK598809 (GSK 598809, GSK-598809)

货号: PC-60743Not For Human Use, Lab Use Only.

GSK598809 (GSK-598809) is a potent, selective, CNS penetrant and orally bioavailable dopamine D3 receptor (D3R) antagonist with pKi of 8.9.

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

    生物&药学活性

    GSK598809 (GSK-598809) is a potent, selective, CNS penetrant and orally bioavailable dopamine D3 receptor (D3R) antagonist with pKi of 8.9.
    GSK598809 displays >100-fold selectivity over D2 and H1 receptors.
    GSK598809 significantly attenuates the expression of conditioned place preference (CPP) to nicotine and cocaine.
    GSK598809 potentiates the hemodynamic effects of cocaine in dogs, also increases mean arterial blood pressure and heart rate in vivo.

    物理化学性质&存储条件

    分子量 481.514
    分子式 C22H23F4N5OS
    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-[2-Fluoro-4-(trifluoromethyl)phenyl]-3-[3-[[4-methyl-5-(4-methyl-1,3-oxazol-5-yl)-4H-1,2,4-triazol-3-yl]thio]propyl]-3-azabicyclo[3.1.0]hexane

    参考文献

    1. Micheli F, et al. J Med Chem. 2010 Jan 14;53(1):374-91.

    2. Appel NM, et al. J Pharmacol Exp Ther. 2015 Sep;354(3):484-92.

    3. Dodds CM, et al. Appetite. 2012 Aug;59(1):27-33.

    4. Searle G, et al. Biol Psychiatry. 2010 Aug 15;68(4):392-9.

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