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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.
MK-8245 displays highly selective over the Δ-5 and Δ-6 desaturases (IC50>100 uM).
MK-8245 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 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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