CCG258208

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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。

CAS NO:

2055990-90-2

GRKs-IN-1

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.