CCG258747

Overview

CCG258747 is a selective GRK2 inhibitor ( IC 50 = 18 nM) with high selectivity over GRK1, GRK5, PKA , and ROCK1 (518, 83, > 5500, and > 550-fold, respectively). CCG258747 also blocks the internalization of the µ-opioid receptor ( MOR ). CCG258747 attenuates IgE mediated anaphylaxis by inhibiting GRK2 and FcεRI signaling pathway but activates mast cells via MRGPRX2 and MRGPRB2 . CCG258747 can be used to study diseases related to overexpression of GRK2 (such as heart failure, opioid tolerance).

Application

Products | Products > Disease Areas > Inflammation or Immune System Disease | Products > Disease Areas > Cardiovascular Disease | Products > Disease Areas > Lipid Metabolism | Products > Disease Areas > Pain | Products > Disease Areas > Hypertension | Products > Disease Areas > Obesity | Products > Disease Areas > Neurological, Eye or Ear Disease | Products > Disease Areas > Blood or Cardio-cerebrovascular Disease | Products > Disease Areas > Metabolic or Endocrine Disease | Products > Signaling Pathways > GPCR/G Protein | Products > Signaling Pathways > Neuronal Signaling | Products > Research Areas > Inflammation/Immunology | Products > Research Areas > Cardiovascular Disease | Products > Signaling Pathways > Opioid Receptor | Products > Signaling Pathways > G Protein-coupled Receptor Kinase (GRK) | Products > Signaling Pathways > Mas-related G-protein-coupled Receptor (MRGPR)

Product Information

• Catalog No.: HY-139690
• CAS No.: 2615910-00-2
• Molecular Formula: C28H27FN4O4
• Molecular Weight: 502.54
• Purity: 98.96%
• Storage: 4°C, sealed storage, away from moisture and light * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
• Solubility: ≥ 2.5 mg/mL (4.97 mM); Clear solution
• Availability: In-stock

Source

Original product source