For research use only. Not for therapeutic Use.
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. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure[1].
| Catalog Number | I044168 |
| CAS Number | 2615910-00-2 |
| Synonyms | 5-[(3S,4R)-3-(1,3-benzodioxol-5-yloxymethyl)piperidin-4-yl]-2-fluoro-N-(2H-indazol-3-ylmethyl)benzamide |
| Molecular Formula | C28H27FN4O4 |
| Purity | ≥95% |
| InChI | InChI=1S/C28H27FN4O4/c29-23-7-5-17(11-22(23)28(34)31-14-25-21-3-1-2-4-24(21)32-33-25)20-9-10-30-13-18(20)15-35-19-6-8-26-27(12-19)37-16-36-26/h1-8,11-12,18,20,30H,9-10,13-16H2,(H,31,34)(H,32,33)/t18-,20-/m0/s1 |
| InChIKey | KGSBEYKVWODBRD-ICSRJNTNSA-N |
| SMILES | C1CNCC(C1C2=CC(=C(C=C2)F)C(=O)NCC3=C4C=CC=CC4=NN3)COC5=CC6=C(C=C5)OCO6 |
| Reference | [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. |
