701232-94-2
Chemical Structure
JTT-553
- CAS No.: 701232-94-2
- Formula:C25H27F3N4O3
- Molecular Weight:488.50
IUPAC Name: 2-((1r,4s)-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
InChIKey: YFJNLPDVCDNOMJ-OJPDTXNBSA-N
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
Biological Activity: 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].
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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). | |||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
