GRK2-IN-1

Modify Date: 2024-01-29 18:48:33

GRK2-IN-1 Structure
GRK2-IN-1 structure
Common Name GRK2-IN-1
CAS Number 2055990-90-2 Molecular Weight 452.48
Density N/A Boiling Point N/A
Molecular Formula C24H25FN4O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of GRK2-IN-1


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].

 Names

Name GRK2-IN-1

 GRK2-IN-1 Biological Activity

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.

 Chemical & Physical Properties

Molecular Formula C24H25FN4O4
Molecular Weight 452.48