GRKs-IN-1 hydrochloride，化合物14as，对 G 蛋白偶联受体激酶 2 GRK2 具有显着的效力和选择性(IC50=130 nM) 和 GRK5 (IC50=7.1 μM)。GRKs-IN-1 hydrochloride 是帕罗西汀的衍生物，与帕罗西汀相比，心肌细胞收缩性测定显示改善了 100 倍。
GRKs-IN-1 hydrochloride, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=130 nM) and GRK5 (IC50=7.1 μM).GRKs-IN-1 hydrochloride is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine[1].
[1]. Waldschmidt HV, et al. Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2Inhibitors Based on Paroxetine. J Med Chem. 2017 Apr 13;60(7):3052-3069.
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