2615910-00-2
Chemical Structure
CCG258747
- CAS No.: 2615910-00-2
- Formula:C28H27FN4O4
- Molecular Weight:502.54
IUPAC Name: N-((1H-indazol-3-yl)methyl)-5-((3S,4R)-3-((benzo[d][1,3]dioxol-5-yloxy)methyl)piperidin-4-yl)-2-fluorobenzamide
InChIKey: KGSBEYKVWODBRD-ICSRJNTNSA-N
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
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
CCG258747 | 98.96% | 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). | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
- [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. [Content Brief]
- [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. [Content Brief]
Keywords
