Products Details

Product Description

– 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].

Web ID

– HY-109562

Shipping

– Room temperature

Applications

– Neuroscience-Neuromodulation

Molecular Formula

– C24H25FN4O4

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.

CAS Number

– 2055990-90-2

Molecular Weight

– 452.48

SMILES

– FC1=C(C(NCC2=NNC=C2)=O)C=C([C@H]3[C@H](COC4=CC=C(OCO5)C5=C4)CNCC3)C=C1

Clinical Information

– No Development Reported

Research Area

– Cardiovascular Disease

Solubility

– 10 mM in DMSO

Target

– G Protein-coupled Receptor Kinase (GRK)

Pathway

– GPCR/G Protein

Product type

– Reference compound

Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.

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