JNJ-DGAT2-A

• CAT Number: I011227
• CAS Number: 1962931-71-0
• Molecular Formula: C24H16BrFN4O2S
• Molecular Weight: 523.38
• Purity: ≥95%
• Synonyms: 3-bromo-4-[2-fluoro-4-[(Z)-[4-oxo-2-(2-pyridin-2-ylethylimino)-1,3-thiazolidin-5-ylidene]methyl]phenoxy]benzonitrile
• InChI: InChI=1S/C24H16BrFN4O2S/c25-18-11-16(14-27)5-6-20(18)32-21-7-4-15(12-19(21)26)13-22-23(31)30-24(33-22)29-10-8-17-3-1-2-9-28-17/h1-7,9,11-13H,8,10H2,(H,29,30,31)/b22-13-
• InChIKey: ZFRHAMOJHTZHLT-XKZIYDEJSA-N
• SMILES: C1=CC=NC(=C1)CCN=C2NC(=O)C(=CC3=CC(=C(C=C3)OC4=C(C=C(C=C4)C#N)Br)F)S2

JNJ-DGAT2-A is a selective diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 value of 0.14 μM in human DGAT2-expressing Sf9 insect cell membranes. JNJ-DGAT2-A can be used for the research of triglyceride (TG) synthesis[1].
JNJ-DGAT2-A (5 μM) inhibits about 99% of recombinant DGAT2 enzymatic activity[1].
JNJ-DGAT2-A (5 μM) inhibits the DGAT activity in HepG2 cell lysates[1].
JNJ-DGAT2-A (0.3125, 0.625, 1.25, 2.5, 5, 10, and 20 µM; 60 min prior to isotope-labeled and additional 2 h after isotope-labeled) dose-dependently inhibits the generation of TG (52:2), TG (54:3), and TG (50:2) using 13C3-D5-glycerol as a substrate in HepG2 cells with IC50 values of 0.85 μM, 0.99 μM, and 0.66 μM, respectively[1].

Reference

[1]. Qi J, et al. The use of stable isotope-labeled glycerol and oleic acid to differentiate the hepatic functions of DGAT1 and -2. J Lipid Res. 2012 Jun;53(6):1106-16.
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