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Art. -Nr.: HY-109562

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CCG258208

(Synonyms: GRKs-IN-1)

1 Cited Publications

Kundenbewertung

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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2055990-90-2
Formel: C₂₄H₂₅FN₄O₄
Molecular Weight:452.48

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

CCG258208 Chemical Structure

CAS. Nr.: 2055990-90-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

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.

Chemical Information

CAS. Nr. 2055990-90-2
Molecular Weight 452.48
Formel C₂₄H₂₅FN₄O₄
SMILES

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

GRKs-IN-1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (1)

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Journal Impact Factor

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Waldschmidt HV, et al. Structure-Based Design of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2Inhibitors Based on Paroxetine. J Med Chem. 2017 Apr 13;60(7):3052-3069. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

CCG258208

1 Cited Publications

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Reinheit & Dokumentation
Verweise

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CCG258208

Publications Citing Use of MedChemExpress (MCE) CCG258208

Biologische Aktivität

Chemical Information

Publications (1)

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

CCG258208 Related Classifications

HY-109562 Related Classifications