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MK-8245
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MK-8245图片
CAS NO:1030612-90-8
规格:98%
分子量:467.25
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
200mg电议

产品介绍
SCD inhibitor,potent and liver-selective
CAS:1030612-90-8
分子式:C17H16BrFN6O4
分子量:467.25
纯度:98%
存储:Store at -20°C

Background:

MK-8245 is a potent and liver-selective inhibitor of stearoyl-CoA desaturase (SCD) with IC50 value of 1nM [1].


SCD1 represents a therapeutic target for the treatment of type II diabetes, dyslipidemia, obesity, and metabolic diseases. As an inhibitor of SCD1, MK-8245 shows potency in both the rat enzyme and hepatocyte assay. There are no significant differences in potencies between the rat, mouse, and human SCD1. MK-8245 is developed as a liver-targeting SCD inhibitor. It demonstrates a liver-targeted tissue distribution profile resulting from a substrate recognition by organic anionic transporter proteins (OATPs) [1, 2].


MK-8245 is effective at lowering glucose level. It can improve glucose clearance dose-dependently with ED50 value of 7mg/kg. In the chronic eDIO mouse study, MK-8245 shows prevention of body weight gain with the maximally efficacious dose of 20 mg/kg bid based on body weight and liver triglyceride reduction [1].


Reference:
[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, Srensen 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.
[2] Lachance N, Guiral S, Huang Z, Leclerc JP, Li CS, Oballa RM, Ramtohul YK, Wang H, Wu J, Zhang L.  Discovery of potent and liver-selective stearoyl-CoA desaturase (SCD) inhibitors in an acyclic linker series. Bioorg Med Chem Lett. 2012 Jan 1;22(1):623-7.