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CCG215022
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。
CCG215022图片
CAS NO:1813527-81-9
规格:98%
分子量:499.5
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 uM, 0.38±0.06 uM and 3.9±1 uM for GRK2, GRK5 and GRK1, respectively.
CAS:1813527-81-9
分子式:C26H22FN7O3
分子量:499.5
纯度:98%
存储:Store at -20°C

Background:

CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 uM, 0.38±0.06 uM and 3.9±1 uM for GRK2, GRK5 and GRK1, respectively.


CCG215022 has nanomolar potency against both GRK2 and GRK5 and is at least 20-fold more potent than Paroxetine. In the course of a GRK2 structure-based drug design campaign, CCG215022 exhibits nanomolar IC50 values against both GRK2 and GRK5 and good selectivity against other closely related kinases such as GRK1 and PKA. Treatment of murine cardiomyocytes with CCG215022 results in significantly increases contractility at 20-fold lower concentrations than Paroxetine, an inhibitor with more modest selectivity for GRK2[1].


参考文献:
[1]. Homan KT, et al. Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally DesignedInhibitor. J Biol Chem. 2015 Aug 21;290(34):20649-59.