Description
MK-8245 is an liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 values of 1 nM, 3 nM and 3 nM for human, rat and mouse SCD1.
Product Overview
MK-8245 is a potent and liver-selective inhibitor of stearoyl-CoA desaturase (SCD) with IC50 value of 1nM. 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). 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.
Molecular Formula
C17H16BrFN6O4
Chemical Name
2-[5-[3-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,2-oxazol-5-yl]tetrazol-2-yl]acetic acid
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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