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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-ME3183
ME3183

Chemical Structure : ME3183

CAS No.: 2231329-25-0

ME3183 (ME 3183)

货号: PC-21464Not For Human Use, Lab Use Only.

ME3183 is a potent, selective phosphodiesterase 4 (PDE4) inhibitor with IC50 of 2.33, 1.28 and 1.63 nM for PDE4B1, PDE4A1A and PDE4D2 respectively.

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

    生物&药学活性

    ME3183 is a potent, selective phosphodiesterase 4 (PDE4) inhibitor with IC50 of 2.33, 1.28 and 1.63 nM for PDE4B1, PDE4A1A and PDE4D2 respectively.
    ME3183 exhibits >194-fold selectivity over other PDEs.
    ME3183 potently inhibits LPS-induced TNF-α, IL-12/23p40, and IL-23 production in PBMCs with IC50 of 0.648, 1.96 and 98.4 nM respectively.
    ME3183 provides superior inhibition of the production of psoriasis-related cytokines, such as TNF-α, IL-12/23p40, IL-23, and IL-17A, by human PBMCs and T cells, compared with apremilast, roflumilast, and crisaborole.
    ME3183 provides superior inhibition of the production of Th2 cytokines, such as IL-4, IL-5, and IL-13, by human T cells.
    ME3183 inhibits ear swelling and cytokine production in skin lesions of mice with chronic oxazolone-induced dermatitis with ED50 of 1.43 mg/kg.

    物理化学性质&存储条件

    分子量 422.45
    分子式 C19H20F2N4O3S
    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

    1-((2-(3,6-diazabicyclo [3.1.1]heptan-3-yl)-7-(thiazol-2-yl)benzo [d]oxazol-4-yl)oxy)-1,1-difluoro-2-methylpropan-2-ol

    参考文献

    1. Kubota-Ishida N, et al. Eur J Pharmacol. 2023 Nov 22;962:176202.

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