MedKoo product information:

MK-8245

MK-8245  is a stearoyl-CoA desaturase (SCD) inhibitor with preclinical antidiabetic and antidyslipidemic efficacy with a significantly improved therapeutic window. MK-8245 is currently being developed by MercK.

MK-8245, a liver-targeted SCD inhibitor believed to inhibit the SCD enzyme solely in the liver and not in other tissues for the following reasons. When SCD inhibition has been measured by desaturation index in tissues of rodents treated with MK-8245, the desaturation index was significantly reduced in liver but not in other tissues such as skin, eye and adipose tissue. 

1: Oballa RM, Belair L, Black WC, Bleasby K, Chan CC, Desroches C, Du X, Gordon R, Guay J, Guiral S, Hafey MJ, Hamelin E, Huang Z, Kennedy B, Lachance N, Landry F, Li CS, Mancini J, Normandin D, Pocai A, Powell DA, Ramtohul YK, Skorey K, Sørensen D, Sturkenboom W, Styhler A, Waddleton DM, Wang H, Wong S, Xu L, Zhang L. 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. PubMed PMID: 21661758.

2: Landry F, Chan CC, Huang Z, Leclair G, Li CS, Oballa R, Zhang L, Bateman K. Plasma-based approach to measure target engagement for liver-targeting stearoyl-CoA desaturase 1 inhibitors. J Lipid Res. 2011 Aug;52(8):1494-9. Epub 2011 Jun 5. PubMed PMID: 21642745; PubMed Central PMCID: PMC3137014.