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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-TRP Channel-AS1928370
AS1928370

Chemical Structure : AS1928370

CAS No.: 1345614-89-2

AS1928370 (ASP-8370;ASP8370)

货号: PC-35235Not For Human Use, Lab Use Only.

AS1928370 (ASP8370) is a potent, selective, orally available TRPV1 antagonist with IC50 of 0.51 uM, shows no inhibitory effects on TRPV4, TRPA11, and TRPM8 at 10 uM.

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

    生物&药学活性

    AS1928370 (ASP8370) is a potent, selective, orally available TRPV1 antagonist with IC50 of 0.51 uM, shows no inhibitory effects on TRPV4, TRPA11, and TRPM8 at 10 uM.
    AS1928370 (ASP8370) demonstrates high aqueous solubility (pH6.8, >100 uM), satisfactory stability in human liver microsomes, and reduced CYP3A4 inhibition.
    AS1928370 (ASP8370) improves capsaicin-induced secondary hyperalgesia and mechanical allodynia in an L5/L6 spinal nerve ligation model in rats with respective ED50s of 0.17 and 0.26 mg/kg p.o.

    物理化学性质&存储条件

    分子量 453.586
    分子式 C29H31N3O2
    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

    (R)-N-(1-methyl-2-oxo-1,2,3,4-tetrahydro-7-quinolyl)-2-[(2-methylpyrrolidin-1-yl)methyl]biphenyl-4-carboxamide

    参考文献

    1. Oka H, et al. Bioorg Med Chem. 2018 Jul 23;26(12):3716-3726.

    2. Watabiki T, et al. J Pharmacol Exp Ther. 2011 Mar;336(3):743-50.

    3. Watabiki T, et al. Biol Pharm Bull. 2011;34(7):1105-8.

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