CCG258747 [CAS 2615910-00-2]

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].

[2615910-00-2]

C28H27FN4O4

502.54

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

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

GRK2; μ Opioid Receptor/MOR

10mM

98.96

DMSO : 100 mg/mL (ultrasonic)

4°C (Powder, sealed storage, away from moisture and light)

Room Temperature