2055990-90-2

2055990-90-2 structure
2055990-90-2 structure
  • Name: GRK2-IN-1
  • Chemical Name: GRK2-IN-1
  • CAS Number: 2055990-90-2
  • Molecular Formula: C24H25FN4O4
  • Molecular Weight: 452.48
  • Catalog: Research Areas Cardiovascular Disease
  • Create Date: 2019-10-07 20:15:52
  • Modify Date: 2025-08-27 13:25:43
  • GRKs-IN-1, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=30 nM) and GRK5 (IC50=7.1 μM).GRKs-IN-1 is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine[1].

Name GRK2-IN-1
Description GRKs-IN-1, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=30 nM) and GRK5 (IC50=7.1 μM).GRKs-IN-1 is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine[1].
Related Catalog
Target

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.

Molecular Formula C24H25FN4O4
Molecular Weight 452.48
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