| Identification | Back Directory | [Name]
MK-8617 | [CAS]
1187990-87-9 | [Synonyms]
CS-2700
MK-8617
MK 8617;MK8617
N-[BIS(4-METHOXYPHENYL)METHYL]-6-OXO-2-PYRIDAZIN-3-YL-1H-PYRIMIDINE-5-CARBOXAMIDE
N-(bis(4-Methoxyphenyl)Methyl)-4-hydroxy-2-(pyridazin-3-yl)pyriMidine-5-carboxaMide
N-(bis(4-methoxyphenyl)methyl)-6-oxo-2-(pyridazin-3-yl)-1,6-dihydropyrimidine-5-carboxamide
5-Pyrimidinecarboxamide,N-[bis(4-methoxyphenyl)methyl]-1,6-dihydro-6-oxo-2-(3-pyridazinyl)- | [Molecular Formula]
C24H21N5O4 | [MDL Number]
MFCD22572348 | [MOL File]
1187990-87-9.mol | [Molecular Weight]
443.45 |
| Chemical Properties | Back Directory | [density ]
1.32±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:5.67(Max Conc. mg/mL);12.79(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.56(Max Conc. mM)
DMF:1.0(Max Conc. mg/mL);2.25(Max Conc. mM) | [form ]
A solid | [pka]
5.54±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
MK-8617 is a potent, selective and bioavailable hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) inhibitor used in the treatment of anemia. | [in vivo]
Tritiated MK-8617 exhibits minimal metabolic turnover in liver microsomes from rat, dog, and monkey (<10% turover) but significant turnover in human liver microsomes (34% turnover) after 60 min (10 μM MK-8617, 1 mg/mL microsomal protein). In terms of its pharmacokinetic profile, MK-8617 shows good oral bioavailability across species (36 to 71%), with low clearance and volume of distribution. After 48 h treatment of MK-8617, postdose recovery of the radioactivity is about 26% bile, 12% urine, and 38% in feces, indicating that ~38% of the MK-8617 is absorbed and eliminated into bile and urine which is consistent with the oral bioavailability (~36%) observed in the rat study. MK-8617 also elicits an increase in erythropoietin (EPO) levels with a mouse MED of 1.5 mpk when dosed iv[1]. |
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