| Identification | Back 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 |
| Hazard Information | Back 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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| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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