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首页-小分子抑制剂&激动剂-GPCR-Adenosine Receptor-ASP5854
ASP5854

Chemical Structure : ASP5854

CAS No.: 851087-60-0

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ASP5854 (ASP-5854)

货号: PC-20111Not For Human Use, Lab Use Only.

ASP5854 (ASP-5854) is a potent adenosine A(1) and A(2A) receptor dual antagonist with binding Ki of 9.03 and 1.76 nM for human A(1) and A(2A) receptors, respectively.

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

    生物&药学活性

    ASP5854 (ASP-5854) is a potent adenosine A(1) and A(2A) receptor dual antagonist with binding Ki of 9.03 and 1.76 nM for human A(1) and A(2A) receptors, respectively.
    ASP5854 displays high specificity over adenosine A3 receptor, and shows similar binding affinity for A1 and A2A receptors in humans, rats, and mice.
    ASP5854 showed antagonistic action on A(1) and A(2A) agonist-induced (CPA, CGS21680) increases of intracellular Ca(2+) concentration with IC50 of 59.81 and 4.21 nM, respectively.
    ASP5854 significantly potentiated l-dihydroxyphenylalanine (L-DOPA)-induced rotational behavior at doses higher than 0.032 mg/kg in unilateral 6-hydroxydopamine-lesioned rats.
    ASP5854 significantly reversed the scopolamine-induced memory deficits in the rat passive avoidance test, but the specific adenosine A(2A) antagonist KW-6002 (istradefylline, Cat#PC-42728) did not.
    ASP5854 ameliorated MK-801-induced impairment of spontaneous alternation in the mouse Y-maze test, but not KW-6002 (istradefylline, Cat#PC-42728).

    物理化学性质&存储条件

    分子量 324.36
    分子式 C18H17FN4O
    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

    5-[5-amino-3-(4-fluorophenyl) pyrazin-2-yl]-1-isopropylpyridine-2(1H)-one

    参考文献

    1. Mihara T, et al. J Pharmacol Exp Ther. 2007 Nov;323(2):708-19.

    2. Mihara T, et al. Behav Brain Res. 2008 Dec 12;194(2):152-61.

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