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 FcepsilonRI 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].
Molecular Weight:
502.54
Purity:
98.96
CAS Number:
[2615910-00-2]
Formula:
C28H27FN4O4
Target:
G Protein-coupled Receptor Kinase (GRK),Mas-related G-protein-coupled Receptor (MRGPR),Opioid Receptor
Application Notes:
MCE Product type: Reference compound
* VAT and and shipping costs not included. Errors and price changes excepted
