CAS:1030612-90-8
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:Light yellow to yellow Solid
MK-8245是肝靶向的硬脂酰-CoA去饱和酶(SCD)抑制剂。
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MK-8245CAS:1030612-90-8
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:Light yellow to yellow Solid
CAS | 1030612-90-8 |
English Name | MK-8245 |
Synonyms | 5-[3-[4-(2-溴-5-氟苯氧基)-1-哌啶基]-5-异恶唑基]-2H-四氮唑-2-乙酸;MK8245 |
Molecular Formula | C17H16BrFN6O4 |
Molecular Weight | 467.26 |
Solubility | Soluble in DMSO |
Purity | ≥98% |
Appearance | Light yellow to yellow Solid |
Storage | Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
MDL | MFCD20039622 |
SMILES | O=C(CN1N=C(N=N1)C2=CC(N3CCC(CC3)OC4=CC(F)=CC=C4Br)=NO2)O |
Target Point | Stearoyl-CoA Desaturase (SCD) |
Passage | Metabolic Enzyme&Protease |
Background | MK-8245 is a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor. |
Biological Activity | MK-8245 is a potent, liver-targeted stearoyl-CoA desaturase (SCD) inhibitor, with IC50s of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with antidiabetic and antidyslipidemic efficacy[1]. |
IC50 | IC50: 1nM(human SCD1);3nM(rat SCD1);3nM(mouse SCD1)[1] |
In Vitro | MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which contains functional,actives organic anion transporting polypeptides(OATPs)with IC50 of 68 nM,while being only weakly active OATPs in the HepG2 cell assay which is devoid of active with IC50 of ~1 μM[1]. |
In Vivo | MK-8245(10mg/kg; p.o.)exhibits a tissue distribution profile concentrated in the liver,with low exposure in tissues associated with potential adverse events in rats,dogs,and rhesus monkeys[1]. |
Data Literature Source | [1]. Oballa RM,et al. Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.J Med Chem. 2011 Jul 28;54(14):5082-96. Epub 2011 Jun 28. |
Unit | Bottle |
Specification | 2mg 5mg 10mg |
MK-8245是肝靶向的硬脂酰-CoA去饱和酶(SCD)抑制剂。