JTT-553

JTT-553 is a DGAT1 inhibitor (IC50: 2.38 nM) . JTT-553 reduces plasma concentrations of glucose, insulin, non-esterified fatty acids (NEFA), total cholesterol (TC), and hepatic triglycerides (TG) . JTT-553 improves insulin-dependent glucose uptake and glucose intolerance in adipose tissue of DIO mice. JTT-553 reduces TNF-α mRNA levels and increases GLUT4 mRNA levels in adipose tissue of KK-Ay mice. JTT-553 improves adipose tissue insulin resistance and systemic glucose metabolism by reducing body weight. JTT-553 can be used in the study of obesity and type 2 diabetes mellitus (T2DM) [1][2].

Product Specifications

CAS Number

[701232-94-2]

UNSPSC

12352005

Target

Acyltransferase

Related Pathways

Metabolic Enzyme/Protease

Field of Research

Metabolic Disease

Smiles

OC(C[C@H]1CC[C@@]2(CC1)C3=CC=C(C4=NC5=C(N)N=C(C(F)(F)F)N=C5OC4(C)C)C=C3CC2)=O

Molecular Formula

C25H27F3N4O3

Molecular Weight

488.50

References & Citations

[1]Tomimoto D, et al. JTT-553, a novel Acyl CoA:diacylglycerol acyltransferase (DGAT) 1 inhibitor, improves glucose metabolism in diet-induced obesity and genetic T2DM mice. J Pharmacol Sci. 2015 Sep;129 (1) :51-8.|[2]Tomimoto D, et al. Pharmacological characterization of [trans-5'- (4-amino-7,7-dimethyl-2-trifluoromethyl-7H-pyrimido[4,5-b][1,4]oxazin-6-yl) -2',3'-dihydrospiro (cyclohexane-1,1'-inden) -4-yl]acetic acid monobenzenesulfonate (JTT-553), a novel acyl CoA:diacylglycerol transferase (DGAT) 1 inhibitor. Biol Pharm Bull. 2015;38 (2) :263-9.