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CCG258208 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CCG258208 hydrochloride图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
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。
别名GRK2-IN-1 hydrochloride
分子式C24H26ClFN4O4
分子量488.94
溶解度DMSO : 250 mg/mL (511.31 mM; Need ultrasonic)|Water : 50 mg/mL (102.26 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.