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
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture and light)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
GRK2; μ Opioid Receptor/MOR
Available Sizes
Frequently Asked Questions
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