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首页-小分子抑制剂&激动剂-GPCR-Prostaglandin Receptor-ONO-4578
ONO-4578

Chemical Structure : ONO-4578

CAS No.: 1965316-82-8

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ONO-4578 (BMS-986310, ONO 4578, BMS 986310)

货号: PC-20853Not For Human Use, Lab Use Only.

ONO-4578 (BMS-986310) is a potent, highly selective EP4 antagonist, potently inhibits the PGE2-induced cAMP production in CHO cells expressing mouse and human EP4 receptors with single-digit nM IC50.

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

    生物&药学活性

    ONO-4578 (BMS-986310) is a potent, highly selective EP4 antagonist, potently inhibits the PGE2-induced cAMP production in CHO cells expressing mouse and human EP4 receptors with single-digit nM IC50.
    ONO-4578 (BMS-986310) shows excellent pharmacokinetic properties after oral dosing in mouse.
    ONO-4578 (BMS-986310) reverses PGE2-mediated suppression of T cell activation and promotes DC differentiation in vitro.
    ONO-4578 (BMS-986310) inhibits growth of CT26 and MC38 tumors in syngeneic mouse, significantly prolongs survival of mice with highly aggressive SB28 gliomas in the brain.
    ONO-4578 (BMS-986310) reduces infiltration of M2 macrophages in MC38 tumors compared with control mice.
    A combination of ONO-4578 (BMS-986310) and anti-PD-1 antibody results in enhanced anti-tumor effects in GL261 and MC38 tumor-bearing mice compared with anti-PD-1 monotherapy.

    物理化学性质&存储条件

    分子量 475.55
    分子式 C27H29N3O5
    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

    4-(4-cyano-2-((2'R)-6-(isopropylcarbamoyl)spiro[chromane-4,1'-cyclopropane]-2'-carboxamido)phenyl)butanoic acid

    参考文献

    1. Tohru Kotani, et al. Cancer Res (2020) 80 (16_Supplement): 4443.

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