CCG258208
Based on 1 publication(s) in Google Scholar
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.
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- CAS No.: 2055990-90-2
- Formule: C24H25FN4O4
- Masse moléculaire:452.48
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Publications Citing Use of MedChemExpress (MCE) CCG258208
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Activité biologique
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GRK2 |
GRK2 30 nM (IC50) |
GRK5 7.1 μM (IC50) |
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.
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Cell Line:Mouse cardiomyocytes
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Concentration:0, 0.1, 0.5, and 1 μM
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Incubation Time:10 min
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Result:Showed a significant increase in contractility at a concentration of only 0.1 µM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 mice[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection; 10 mg/kg; once
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Result:Showed total plasma drug levels after single IP administration that exceed the GRK2 IC50 for seven hours.
Chemical Information
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CAS No. 2055990-90-2
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Masse moléculaire 452.48
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Formule C24H25FN4O4
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SMILES
FC1=C(C(NCC2=NNC=C2)=O)C=C([C@H]3[C@H](COC4=CC=C(OCO5)C5=C4)CNCC3)C=C1
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Synonyms
GRKs-IN-1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Commun Biol
Cell-based and isoform-selective G protein-coupled receptor kinase assays for comprehensive inhibitor evaluation. [Abstract]2026 Jan 16;9(1):287. PMID: 41545717
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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