MK-8617

MK-8617 is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 1 (HIF-PH1), HIF-PH2, and HIF-PH3 (IC50s = 1, 1, and 14 nM, respectively). It is selective for HIF-PH1, -2, and -3 over the cytochrome P450 (CYP) isoforms CYP1A2, -3A4, -2B6, -2C9, -2C19, and -2D6 (IC50s = >1.6 µM for all) and factor inhibiting HIF (FIH, IC50 = 18 µM), as well as over a panel of 171 enzymes at 10 µM. MK-8617 (5 and 15 mg/kg) increases serum levels of erythropoietin (EPO) and hemoglobin, as well as the number of circulating red blood cells, in rats.Formal Name: N-[bis(4-methoxyphenyl)methyl]-1,6-dihydro-6-oxo-2-(3-pyridazinyl)-5-pyrimidinecarboxamide. CAS Number: 1187990-87-9. Molecular Formula: C24H21N5O4. Formula Weight: 443.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 1 mg/ml, DMSO: 1 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 231 nm. SMILES: O=C1NC(C2=CC=CN=N2)=NC=C1C(NC(C3=CC=C(C=C3)OC)C4=CC=C(C=C4)OC)=O. InChi Code: InChI=1S/C24H21N5O4/c1-32-17-9-5-15(6-10-17)21(16-7-11-18(33-2)12-8-16)27-23(30)19-14-25-22(28-24(19)31)20-4-3-13-26-29-20/h3-14,21H,1-2H3,(H,27,30)(H,25,28,31). InChi Key: WXLPERVDMILVIF-UHFFFAOYSA-N.