Product Data SheetProduct Name:CAS No.: Cat. No.:MWt:Formula:Purity :MK-8245 Trifluoroacetate1415559-41-9HY-13077581.27C19H17BrF4N6O6>98%Solubility:DMSOMechanisms: Pathways:Metabolism/Protease; Target:SCD Biological Activity:MK8245 trifluoroacetate is a livertargeting inhibitor of stearoylCoA desaturase (SCD) with IC50 ofMK-8245trifluoroacetateisaliver-targetinginhibitorofstearoyl-CoAdesaturase(SCD)withIC50of1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy. IC50 value: 1 nM (hSCD1) [1] Target: SCD1 in vitro: MK-8245, a phenoxy piperidine isoxazole derivative, has been identified as a potent andliver-specific SCD inhibitor. It contains a tetrazole acetic acid moiety, which is the key molecule forOATPs recognition and liver-targeting. MK-8245 displays similar potencies against human, rat andmouse SCD1 with IC50 values of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouseSCD1. MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which containsfunctional, active OATPs with IC50 of 68 nM, while being only weakly active in the HepG2 cell assaywhich is devoid of active OATPs with IC5...References:[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.2011Jul28;54(14):5082-962011 Jul 28;54(14):508296. Epub 2011 Jun 28.Epub2011Jun28 Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com18Wilkinson Way, Princeton, NJ 08540,USAess.com Web: www.medchemexpress.comEmail: info@medchemexpr
