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ASIC1a inhibitor 5b

Chemical Structure : ASIC1a inhibitor 5b

CAS No.: 1787243-08-6

ASIC1a inhibitor 5b

Catalog No.: PC-73335Not For Human Use, Lab Use Only.

ASIC1a inhibitor 5b is a highly selective and potent ASIC1a inhibitor, inhibits proton-evoked ASIC1a currents with an apparent IC50 of 27 nM at pH 6.7.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    ASIC1a inhibitor 5b is a highly selective and potent ASIC1a inhibitor, inhibits proton-evoked ASIC1a currents with an apparent IC50 of 27 nM at pH 6.7.
    ASIC1a inhibitor 5b can potently and selectively inhibit acid-induced activation of ASIC1a-containing channels, including both ASIC1a homotrimers and ASIC1a-ASIC2 heterotrimers, in a pH-dependent manner.
    ASIC1a inhibitor 5b binds to the acidic pocket of ASIC1a, exhibits a dramatic leftward shift under pH 6.7 activation of ASIC1a as compared to pH 6.0.
    ASIC1a inhibitor 5b protected neurons from ASIC1a-dependent cell death and is blood-brain barrier permeable.
    ASIC1a inhibitor 5b (5 mg/kg) attenuated neurological impairment and alleviated infarct volume in mouse MCAO model of ischemic stroke.

    Physicochemical Properties

    M.Wt 499.861
    Formula C23H29Cl3N4O2
    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

    7-((4-chlorobenzyl)(2-(diethylamino)ethyl)amino)-2-oxo-2H-chromene-3-carboximidamide dihydrochloride

    References

    1. Xin Qi, et al. Front Pharmacol. 2022 Mar 24;13:849498.

    2. Andriy Buta, et al. J Med Chem. 2015 Jun 11;58(11):4449-61.

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