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AA6216

Chemical Structure : AA6216

CAS No.: 1644280-85-2

AA6216 (AA 6216)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 418.819
    Formula C16H14ClF3N4O2S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    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

    References

    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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