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首页-小分子抑制剂&激动剂-GPCR-Dopamine Receptor-SB269652
SB269652

Chemical Structure : SB269652

CAS No.: 215802-15-6

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SB269652 (SB 269652;SB-269652)

货号: PC-42975Not For Human Use, Lab Use Only.

SB269652 is a potent, selective, negative allosteric modulator of dopamine D2 and D3 receptors, abolishes specific binding of [3H]nemanopride and [3H]spiperone to CHO-transfected D3 receptors with IC50 of1.86 and 0.18 nM.

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

    生物&药学活性

    SB269652 is a potent, selective, negative allosteric modulator of dopamine D2 and D3 receptors, abolishes specific binding of [3H]nemanopride and [3H]spiperone to CHO-transfected D3 receptors with IC50 of1.86 and 0.18 nM.
    SB269652 potently blocks D3 receptor-mediated activation of Gα(i3) and phosphorylation of ERK1/2 at 1-10 uM, partially (35%) inhibits the dopamine-induced recruitment of β-arrestin2 to D2 receptors.
    SB269652 is actually a negative allosteric modulator of D2- and D3-receptor dimers.

    物理化学性质&存储条件

    分子量 426.5533
    分子式 C27H30N4O
    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

    1H-Indole-2-carboxamide, N-[trans-4-[2-(7-cyano-3,4-dihydro-2(1H)-isoquinolinyl)ethyl]cyclohexyl]-

    参考文献

    1. Shonberg J, et al. J Med Chem. 2015 Jul 9;58(13):5287-307.

    2. Lane JR, et al. Nat Chem Biol. 2014 Sep;10(9):745-52.

    3. Silvano E, et al. Mol Pharmacol. 2010 Nov;78(5):925-34.

    4. Rossi M, et al. Mol Pharmacol. 2017 Jun;91(6):586-594.

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