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

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (CCG258208 hydrochloride) usually boasts enhanced water solubility and stability.

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CCG258208

CCG258208 Estructura química

No. CAS : 2055990-90-2

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CCG258208 Related Antibodies

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Descripciòn

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

 

GRK2

30 nM (IC50)

GRK5

7.1 μM (IC50)

In Vitro

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

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

CCG258208 Related Antibodies

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.
In Vivo

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

MedChemExpress (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.
Peso molecular

452.48

Fòrmula

C24H25FN4O4
No. CAS
SMILES

FC1=C(C(NCC2=NNC=C2)=O)C=C([C@H]3[C@H](COC4=CC=C(OCO5)C5=C4)CNCC3)C=C1
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
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CCG258208 Related Classifications

  • Calculadora de molaridad

  • Calculadora de dilución

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

Keywords:

CCG2582082055990-90-2GRKs-IN-1CCG 258208CCG-258208G Protein-coupled Receptor Kinase (GRK)G protein-coupled receptor kinase 2heart failurecardiomyocytesInhibitorinhibitorinhibit

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Nombre del producto:
CCG258208
Cat. No.:
HY-109562
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