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

Catalog No. M11723 CAS No. 1415559-41-9

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

MK-8245 trifluoroacetate
Note

Research use only, not for human use.
Brief Description

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.
Description

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.
In Vitro

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In Vivo

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Synonyms

MK 8245 Trifluoroacetate | MK8245 Trifluoroacetate
Pathway

Metabolic Enzyme/Protease
Target

SCD
Recptor

SCD
Research Area

Metabolic Disease
Indication

Diabetes

CAS Number

1415559-41-9
Formula Weight

581.2725
Molecular Formula

C19H17BrF4N6O6
Purity

>98% (HPLC)
Solubility

10 mM in DMSO
SMILES

C1CN(CCC1OC2=C(C=CC(=C2)F)Br)C3=NOC(=C3)C4=NN(N=N4)CC(=O)O.C(=O)(C(F)(F)F)O
Chemical Name

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

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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