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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phospholipase-AK106-001616
AK106-001616

Chemical Structure : AK106-001616

CAS No.: 590416-75-4

AK106-001616 (AK 106-001616)

货号: PC-36162Not For Human Use, Lab Use Only.

AK106-001616 (AK 106-001616) is a potent and selective inhibitor of cytosolic phospholipase A2 (cPLA2) with IC50 of 3.8 nM (human cPLA2 enzyme).

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

    生物&药学活性

    AK106-001616 (AK 106-001616) is a potent and selective inhibitor of cytosolic phospholipase A2 (cPLA2) with IC50 of 3.8 nM (human cPLA2 enzyme).
    AK106-001616 also inhibited rat cPLA2 with IC50 of 4.3 nM, shows no significant activity against human iPLA2, bovine sPLA2 IB and PAF-AH (>10,000 fold selectivity).
    AK106-001616 suppressed the release of AA from Ca2+ ionophore A23187-stimulated rat RBL-2H3 cells (IC50=5.5 nM), also suppressed the production of PGE2 by LPS-stimulated human PBMCs (IC50=5.1 nM) and the production of LTB4 by Ca2+ ionophore A23187-stimulated RBL-2H3 cells (IC50=2.6 nM).
    AK106-001616 demonstrates in vivo efficacy for inflammation, neuropathic pain, and pulmonary fibrosis.

    物理化学性质&存储条件

    分子量 427.504
    分子式 C26H25N3O3
    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

    3-(3-amino-4-((2,3-dihydro-1H-inden-2-yl)oxy)-5-(1-methyl-1H-indazol-5-yl)phenyl)propanoic acid

    参考文献

    1. Shimizu H, et al. J Pharmacol Exp Ther. 2019 Apr 10. pii: jpet.118.255034.

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