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.

For research use only. We do not sell to patients.

CCG258208 Chemical Structure

CCG258208 Chemical Structure

CAS No. : 2055990-90-2

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CCG258208 Related Antibodies

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Description

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)

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.
Molecular Weight

452.48

Formula

C24H25FN4O4
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CCG258208 Related Classifications

  • Molarity Calculator

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The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
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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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