CCG-215022

CCG-215022 is a G protein-coupled receptor kinase (GRK) inhibitor (IC50s = 3.9, 0.15, and 0.38 µM for GRK1, GRK2, and GRK5, respectively). It is selective for GRKs over protein kinase A (PKA, IC50 = 120 µM). CCG-215022 (500 nM) increases contractility in isoproterenol-stimulated isolated mouse cardiomyocytes. It prevents the desensitization of histamine H1 receptor- and purinergic P2Y2 receptor-driven phospholipase C signaling in human ULTR myometrial cells and isolated rat mesenteric smooth muscle cells (MSMCs), respectively (IC50s = 3.09 and 2.95 µM, respectively).Formal Name: 4-[4-fluoro-3-[[(2-pyridinylmethyl)amino]carbonyl]phenyl]-1,2,3,4-tetrahydro-N-1H-indazol-5-yl-6-methyl-2-oxo-5-pyrimidinecarboxamide. CAS Number: 1813527-81-9. Molecular Formula: C26H22FN7O3. Formula Weight: 499.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 1 mg/ml, DMSO:PBS (pH 7.2) (1:5): 0.16 mg/ml. SMILES: O=C1NC(C)=C(C(NC2=CC(C=NN3)=C3C=C2)=O)C(C4=CC(C(NCC5=CC=CC=N5)=O)=C(F)C=C4)N1. InChi Code: InChI=1S/C26H22FN7O3/c1-14-22(25(36)32-17-6-8-21-16(10-17)12-30-34-21)23(33-26(37)31-14)15-5-7-20(27)19(11-15)24(35)29-13-18-4-2-3-9-28-18/h2-12,23H,13H2,1H3,(H,29,35)(H,30,34)(H,32,36)(H2,31,33,37). InChi Key: BLMBNKDQXGINRE-UHFFFAOYSA-N.