1. GPCR/G Protein
  2. G Protein-coupled Receptor Kinase (GRK)
  3. CCG258208

CCG258208  (Synonyms: GRKs-IN-1)

目录号: HY-109562
产品使用指南

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。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 CCG258208 hydrochloride 通常具有更好的水溶性和稳定性。

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CCG258208 Chemical Structure

CCG258208 Chemical Structure

CAS No. : 2055990-90-2

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CCG258208 的其他形式现货产品:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CCG258208 (GRK2-IN-1) is a potent and selective GRK2 (G protein-coupled receptor kinase 2) 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, and ROCK1. 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC50 for seven hours.
分子量

452.48

Formula

C24H25FN4O4

CAS 号
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.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
CCG258208
目录号:
HY-109562
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