Takeda-103A

Takeda-103A is an inhibitor of G protein-coupled receptor kinase 2 (GRK2). It selectively inhibits phosphorylation of bovine rod outer segments by GRK2 (IC50 = 54 nM) over phosphorylation by GRK1 and GRK5 at concentrations up to 125 µM. Takeda-103A also inhibits phosphorylation of bovine rod outer segments by GRK2 containing various mutations, including GRK2L271M, GRK2Y206S, GRK2I197L, and GRK2L235G (IC50s = 24, 55, 106, and 180 nM, respectively).Formal Name: N-[(2,6-difluorophenyl)methyl]-3-[[[4-propyl-5-(4-pyrimidinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-benzamide. CAS Number: 865609-72-9. Molecular Formula: C24H23F2N7O. Formula Weight: 463.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml, Ethanol: Soluble: >10 mg/ml. SMILES: O=C(C1=CC(NCC2=NN=C(C3=NC=NC=C3)N2CCC)=CC=C1)NCC4=C(F)C=CC=C4F. InChi Code: InChI=1S/C24H23F2N7O/c1-2-11-33-22(31-32-23(33)21-9-10-27-15-30-21)14-28-17-6-3-5-16(12-17)24(34)29-13-18-19(25)7-4-8-20(18)26/h3-10,12,15,28H,2,11,13-14H2,1H3,(H,29,34). InChi Key: VWBSMGFTNCQOMB-UHFFFAOYSA-N.