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31120

CCG-215022

Cayman Chemical

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DETAILS

  • Inchi: 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)
  • Purity: ≥98%
  • Raptas: Product Type|Biochemicals|Kinase Inhibitors|GRKs||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cardiovascular System|Heart|Myocardial Contractility||Research Area|Cardiovascular System|Vasculature|Smooth Muscle Cells
  • 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
  • Inchikey: BLMBNKDQXGINRE-UHFFFAOYSA-N
  • Cas Number: 1813527-81-9
  • Formulation: A crystalline solid
  • Storage Temp: -20
  • Shipping Temp: -20
  • Formula Markup: C26H22FN7O3
  • Formula Weight: 499.5
  • Shelf Life Days: 1460

DESCRIPTION

A GRK inhibitor (IC50s = 3.9, 0.15, and 0.38 μM for GRK1, GRK2, and GRK5, respectively); selective for GRKs over PKA (IC50 = 120 μM); increases contractility in isoproterenol-stimulated isolated mouse cardiomyocytes at 500 nM; prevents the desensitization of histamine H1 receptor- and purinergic P2Y2 receptor-driven phospholipase C signaling in human ULTR myometrial cells and isolated rat MSMCs, respectively (IC50s = 3.09 and 2.95 μM, respectively)