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Supplier NameMedChemExpress (MCE)
Contactsales
Tel609-228-6898
Mobile609-228-6898
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Emailsales@medchemexpress.com; tech@medchemexpress.com
Websitehttps://www.medchemexpress.com/
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Product NameGRK2-IN-1
SynonymsGRK2-IN-1;CCG258208;Benzamide, 5-[(3S,4R)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-piperidinyl]-2-fluoro-N-(1H-pyrazol-3-ylmethyl)-
CAS2055990-90-2
EINECS
Chemical FormulaC24H25FN4O4
Molecular Weight452.48
inchi
PackageInquiry
PriceGet quote
DescriptionsCCG258208

CCG258208

MedChemExpress (MCE)

HY-109562

2055990-90-2

GRKs-IN-1

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

Room temperature in continental US

Descriptions

CCG258208

CCG258208

MedChemExpress (MCE)

HY-109562

2055990-90-2

GRKs-IN-1

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

Room temperature in continental US
may vary elsewhere.

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.

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

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

GRK2 30 nM (IC50) GRK5 7.1 μM (IC50)

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[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]

Supplier Websitehttps://www.medchemexpress.com/grk2-in-1.html
Last Update2025-05-21 16:50:25
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