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CCG258208
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图片
CAS NO:2055990-90-2
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
GRKs-IN-1
产品介绍
CCG258208 (GRK2-IN-1) 是一种强效和选择性的GRK2(G蛋白偶联受体激酶2) 抑制剂 (IC50=30 nM),对 GRK5 (IC50=7.09 μM) 显示出 230 倍的选择性,对 GRK1 (IC50=87.3 μM)、PKA 和 ROCK1 有超过 2500 倍的选择性。CCG258208 可用于心衰的研究。
生物活性

CCG258208 (GRK2-IN-1) is a potent and selectiveGRK2(G protein-coupled receptor kinase2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM),PKA, andROCK1. CCG258208 can be used in heart failure research[1].

IC50& Target

GRK2

30 nM (IC50)

GRK5

7.1 μM (IC50)

体外研究
(In Vitro)

CCG258208 (Compound 14as) (0-1 μM; 10 min) shows significant improvement in βAR-stimulated contractility in mouse cardiomyocytes[1].

Cell Viability Assay[1]

Cell Line:Mouse cardiomyocytes
Concentration:0, 0.1, 0.5, and 1 μM
Incubation Time:10 min
Result:Showed a significant increase in contractility at a concentration of only 0.1 μM.
体内研究
(In Vivo)

CCG258208 (Compound 14as) (intraperitoneal injection; 10 mg/kg; once) treatment shows superior half-life in vivo[1].

Animal Model:CD-1 mice[1]
Dosage:10 mg/kg
Administration:Intraperitoneal injection; 10 mg/kg; once
Result:Showed total plasma drug levels after single IP administration that exceed the GRK2 IC50for seven hours.
分子量

452.48

Formula

C24H25FN4O4

CAS 号

2055990-90-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.