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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-AA6216
AA6216

Chemical Structure : AA6216

CAS No.: 1644280-85-2

AA6216 (AA 6216)

货号: PC-72100Not For Human Use, Lab Use Only.

AA6216 (AA 6216) is novel potent, selective PDE4 inhibitor with IC50 of 0.63 nM.

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

    生物&药学活性

    AA6216 (AA 6216) is novel potent, selective PDE4 inhibitor with IC50 of 0.63 nM.
    AA6216 showed stronger inhibitory effects against PDE4 than other PDE family members.
    AA6216 potently inhibits cytokine production (TNF-α,IL-12p40, IL-4, and IL-13, IC50s=2.2-7.9 nM) by PBMCs stimulated with PHA.
    AA6216 inhibited the production of TGF-β1 by a human monocytic cell line THP-1, AA6216 dose-dependently reduced the production of TNF-α by alveolar macrophages from patients with IPF.
    AA6216 demonstrated anti-fibrotic potency on mouse model of bleomycin-induced lung fibrosis.

    物理化学性质&存储条件

    分子量 418.819
    分子式 C16H14ClF3N4O2S
    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

    (S)-5-chloro-2-(2-methylpiperazin-1-yl)-7-(thiazol-2-yl)-4-(trifluoromethoxy)benzo [d]oxazole

    参考文献

    1. Matsuhira T, et al. Eur J Pharmacol. 2020 Oct 15;885:173508.

    2. Kubota-Ishida N, et al. Eur J Pharmacol. 2021 Sep 5;906:174258.

    3. Matsuhira T, et al. Biochem Biophys Rep. 2021 Aug 28;28:101118.

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