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MK-8245

Chemical Structure : MK-8245

CAS No.: 1030612-90-8

MK-8245 (MK 8245;MK8245)

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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 467.2491
Formula C17H16BrFN6O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 19 mg/mL

Chemical Name/SMILES

2H-Tetrazole-2-acetic acid, 5-[3-[4-(2-bromo-5-fluorophenoxy)-1-piperidinyl]-5-isoxazolyl]-

References

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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