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GRK2-IN-115h hydrochloride

Chemical Structure : GRK2-IN-115h hydrochloride

CAS No.: 1941168-71-3

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GRK2-IN-115h hydrochloride (GRK2 inhibitor 115h hydrochloride)

Catalog No.: PC-60353Not For Human Use, Lab Use Only.

GRK2-IN-115h hydrochloride is a highly potent and selective GRK2 inhibitor with IC50 of 18 nM.

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

    Biological Activity

    GRK2-IN-115h hydrochloride is a highly potent and selective GRK2 inhibitor with IC50 of 18 nM.
    GRK2-IN-115h shows enough selectivity against GRK1/5/6/7, ROCK2 and PKCα with equipotent inhibition to GRK3 (IC50=5.4 nM).
    GRK2-IN-115h potentiates βAR-mediated cAMP accumulation and prevents internalization of βARs in β2AR-expressing HEK293 cells treated with isoproterenol.
    GRK2-IN-115h is a novel potential agent for heart failure treatment.

    Physicochemical Properties

    M.Wt 502.926
    Formula C24H22ClF3N6O
    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

    3-(((4-methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)methyl)amino)-N-(2-(trifluoromethyl)benzyl)benzamide hydrochloride

    References

    1. Okawa T, et al. J Med Chem. 2017 Aug 24;60(16):6942-6990.

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