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MK-8245 trifluoroacetate

Chemical Structure : MK-8245 trifluoroacetate

CAS No.: 1415559-41-9

MK-8245 trifluoroacetate (MK 8245 Trifluoroacetate; MK8245 Trifluoroacetate)

Catalog No.: PC-43378Not For Human Use, Lab Use Only.

MK-8245 trifluoroacetate 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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Biological Activity

MK-8245 trifluoroacetate 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; 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; 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.

Diabetes

Phase 1 Discontinued

Physicochemical Properties

M.Wt 581.2725
Formula C19H17BrF4N6O6
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

10 mM in DMSO

Chemical Name/SMILES

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

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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