Chemical Structure : MK-8245
CAS No.: 1030612-90-8
Catalog No.: PC-43373Not For Human Use, Lab Use Only.
MK-8245 is a potent, selective liver-targeted stearoyl-CoA desaturase (SCD) inhibitor with IC50 of 3, 3 and 1 nM for rat, mouse and human SCD1 enzyme, respectively.
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MK-8245 is a potent, selective liver-targeted stearoyl-CoA desaturase (SCD) inhibitor with IC50 of 3, 3 and 1 nM for rat, mouse and human SCD1 enzyme, respectively.
MK-8245 displays highly selective over the Δ-5 and Δ-6 desaturases (IC50>100 uM); has IC50 values of 68 nM and 1066 nM in Hum HepG2 and rat hepatocyte assays, demonstrates HepG2/hepatocyte ratio of 16:1.
MK-8245 exhibits preclinical antidiabetic and antidyslipidemic efficacy in vivo, demonstrats maximal liver SCD inhibition while sparing inhibition in the skin and eye tissues associated with adverse events.
M.Wt | 467.2491 | |
Formula | C17H16BrFN6O4 | |
Appearance | Solid | |
Storage |
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Solubility |
DMSO: 19 mg/mL |
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Chemical Name/SMILES |
2H-Tetrazole-2-acetic acid, 5-[3-[4-(2-bromo-5-fluorophenoxy)-1-piperidinyl]-5-isoxazolyl]- |
1. Oballa RM, et al. J Med Chem. 2011 Jul 28;54(14):5082-96.
2. Landry F, et al. J Lipid Res. 2011 Aug;52(8):1494-9.
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