CCG258747

CCG258747 is a selective GRK2 inhibitor (IC50 = 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) [1][2].

Product Specifications

CAS Number

[2615910-00-2]

UNSPSC

12352005

Target

G Protein-coupled Receptor Kinase (GRK) ; Mas-related G-protein-coupled Receptor (MRGPR) ; Opioid Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Field of Research

Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/ccg258747.html

Concentration

10mM

Purity

98.96

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(NCC1=NNC2=CC=CC=C12)C(C=C3[C@@](CCNC4)([H])[C@@H]4COC5=CC=C(OCO6)C6=C5)=C(C=C3)F

Molecular Formula

C28H27FN4O4

Molecular Weight

502.54

References & Citations

[1]Renee A Bouley, et al. A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of the μ-Opioid Receptor. Mol Pharmacol. 2020 Jun;97 (6) :392-401.|[2]Thapaliya M, et al. GRK2 inhibitors, paroxetine and CCG258747, attenuate IgE-mediated anaphylaxis but activate mast cells via MRGPRX2 and MRGPRB2. Front Immunol. 2022 Oct 6;13:1032497.