For research purposes only

Cat. No BA94673148

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Description of biological activity

Diacylglycerol acyltransferase (DGAT1) inhibitor. An in vitro assay [WO2007/144571 A1, 2007] to identify DGATl inhibitors used human DGATl expressed in insect cell membranes as the enzyme source. The sf9 cells were infected with recombinant baculovirus containing human DGATl coding sequences and harvested after 48 h. Cells were lysed by sonication and membranes isolated by centrifuging at 28000 rpm for 1 h at 4 °C on a 41% sucrose gradient. The membrane fraction at the interphase was collected, washed, and stored in liquid nitrogen. The compound at 1-10 μM was incubated with 0.4 μg membrane protein, 5 mM MgCl2, and 10 μM 1,2 dioleoyl-sn-glycerol in a total assay volume of 200 μl in plastic tubes. The reaction was started by adding 14C oleoyl coenzyme A (30μM final concentration) and incubated at room temperature for 30 minutes. The reaction was stopped by adding 1.5 mL 2-propanol:heptane:water (80:20:2). Radioactive triolein product was separated into the organic phase by adding 1 mL of heptane and 0.5 mL of 0.1 M carbonate buffer, pH 9.5. DGATl activity was quantified by counting aliquots of the upper heptane layer by liquid scintillography. In this test the compound has an IC50 of 2.5 nM.

Keywords: Inhibitors Obesity

TECHNICAL INFORMATION

(trans-4-{4-[({5-[(3,4-difluorophenyl)amino]-1,3,4-oxadiazol-2-yl}carbonyl)amino]phenyl}cyclohexyl) acetic acid diacylglycerol acyltransferase (DGAT1) inhibitor.

IUPAC Name: (trans-4-{4-[({5-[(3,4-difluorophenyl)amino]-1,3,4-oxadiazol-2-yl}carbonyl)amino]phenyl}cyclohexyl) acetic acid

CAS Number: 892489-52-0

Purity: > 96% chemical purity (LCMS)

1H-NMR spectrum (click to enlarge)

REFERENCES

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