DC Chemicals · Product datasheet

MK-8617 — Datasheet

CAT. NO. DC21288

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ParameterValue
Chemical NameN-(Bis(4-methoxyphenyl)methyl)-4-hydroxy-2-(pyridazin-3-yl)pyrimidine-5-carboxamide
CAS No.1187990-87-9
SynonymsN-(bis(4-methoxyphenyl)methyl)-6-oxo-2-(pyridazin-3-yl)-1,6-dihydropyrimidine-5-carboxamide;N-(bis(4-methoxyphenyl)methyl)-4-hydroxy-2-(pyridazin-3-yl)pyrimidine-5-carboxamide;39RRC0G27V;MK 8617;BCP25371;s8443;AK670649;N-[bis(4-methoxyphenyl)methyl]-6-oxo-2-pyridazin-3-yl-1H-pyrimidine-5-carboxamide;5-Pyrimidinecarboxamide, N-(bis(4-methoxyphenyl)methyl)-1,6-dihydro-6-oxo-2-(3-pyridazinyl)-;N-[Bis(4-methoxyphenyl)methyl]-4-hydroxy-2-(pyridazin-3-yl)pyrimidine-5-carboxamide;5-Pyrimidinecarboxamide, N-(bis(4-methoxypheny;MK-8617
FormulaC24H21N5O4
M.Wt443.4546
SMILESO(C([H])([H])[H])C1C([H])=C([H])C(=C([H])C=1[H])C([H])(C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])[H])N([H])C(C1=C([H])N=C(C2C([H])=C([H])C([H])=NN=2)N([H])C1=O)=O
Purity>97%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2.

In Vitro

MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2. MK-8617 is not a significant inhibitor of the cytochrome p450 enzymes in vitro (IC50), CYP1A2, 3A4, 2B6, 2C9, 2C19, or 2D6, >60 μM, and is a moderate reversible inhibitor of CYP2C8 at 1.6 μM in vitro. The IC50 of MK-8617 is determined for factor inhibiting HIF (FIH) to be 18 μM[1].

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].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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