| Bioactivity | 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]. |
| Target | IC50: 1 nM (human SCD1), 3 nM (rat SCD1), 3 nM (mouse SCD1) |
| Invitro | MK-8245 is a potent and liver-specific SCD inhibitor[1].MK-8245 displays similar potencies against human, rat and mouse SCD1, with IC50 values of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1[1].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].MK-8245 improves glucose clearance in a dose-dependent manner in eDIO mice administrated before the glucose challenge[1]. Animal Model: |
| Name | MK-8245 |
| CAS | 1030612-90-8 |
| Formula | C17H16BrFN6O4 |
| Molar Mass | 467.25 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [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. |
MK-8245
CAS: 1030612-90-8 F: C17H16BrFN6O4 W: 467.25
MK-8245 is a potent, liver-targeted stearoyl-CoA desaturase (SCD) inhibitor, with IC50sof 1 nM for human SCD1 and 3 nM f
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