CCG215022 is a potent GRK2 and GRK5 inhibitor. CCG215022 exhibited 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 resulted in significantly increased contractility at 20-fold lower concentrations than paroxetine, an inhibitor with more modest selectivity for GRK2. G protein-coupled receptor kinases (GRKs) regulate cell signaling by initiating the desensitization of active G protein-coupled receptors. The two most widely expressed GRKs (GRK2 and GRK5) play a role in cardiovascular disease and thus represent important targets for the development of novel therapeutic drugs.
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化学信息
名称 | CCG215022 |
Iupac 化学名称 | CCG215022 |
同义词 | CCG 215022; CCG-215022 |
英文同义词 | CCG 215022; CCG-215022 |
分子式 | C26H22FN7O3 |
分子量 | 499.5064 |
InChiKey | |
InChi | |
Cas号 | 1813527-81-9 |
相关CAS号 | |
外观性状 | crystalline solid |
纯度 | 98% |
存储 | 3 years -20ºCpowder |
可溶性 | Soluble in DMSO |
处理方式 | |
运输条件 | Shipped under ambient temperature as non-hazardous chemical. |
海关编码 | |
Targets | |
Mechanism | |
Cell study | |
Animal study | |
Clinical study | |