MK-8617
MK-8617 Basic information
- Product Name:
- MK-8617
- Synonyms:
-
- N-[BIS(4-METHOXYPHENYL)METHYL]-6-OXO-2-PYRIDAZIN-3-YL-1H-PYRIMIDINE-5-CARBOXAMIDE
- MK 8617;MK8617
- CS-2700
- 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)-
- MK-8617
- N-(bis(4-Methoxyphenyl)Methyl)-4-hydroxy-2-(pyridazin-3-yl)pyriMidine-5-carboxaMide
- MK-8617,MK 8617,HIF-PH,inhibit,Hypoxia-inducible factors,HIFs,Inhibitor,HIF/HIF Prolyl-Hydroxylase
- CAS:
- 1187990-87-9
- MF:
- C24H21N5O4
- MW:
- 443.45
- Mol File:
- 1187990-87-9.mol
MK-8617 Chemical Properties
- 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
MK-8617 Usage And Synthesis
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].
MK-8617Supplier
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- 021-58359326 15900795984
- angsihuaxue@126.com
- Tel
- +86-021-58975553
- sales@cooperpharm.com
- Tel
- 021-52996696，15000506266 15000506266
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- 021-65675885 18964387627
- info@efebio.com
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- 021-61312847; 18021002903
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