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2055990-90-2

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2055990-90-2 Structure

2055990-90-2 Structure
IdentificationBack Directory
[Name]

GRK2-IN-1
[CAS]

2055990-90-2
[Synonyms]

GRK2-IN-1
CCG258208
CCG258208,CCG-258208
Benzamide, 5-[(3S,4R)-3-[(1,3-benzodioxol-5-yloxy)methyl]-4-piperidinyl]-2-fluoro-N-(1H-pyrazol-3-ylmethyl)-
[Molecular Formula]

C24H25FN4O4
[MDL Number]

MFCD32201031
[MOL File]

2055990-90-2.mol
[Molecular Weight]

452.48
Chemical PropertiesBack Directory
[Boiling point ]

660.9±55.0 °C(Predicted)
[density ]

1.314±0.06 g/cm3(Predicted)
[pka]

13.12±0.46(Predicted)
Hazard InformationBack Directory
[Uses]

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].
[in vivo]

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

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.
[IC 50]

GRK2: 30 nM (IC50); GRK5: 7.1 μM (IC50)
[References]

[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. DOI:10.1021/acs.jmedchem.7b00112
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