DGAT-1 inhibitor 2

• CAT Number: I005608
• CAS Number: 942999-61-3
• Molecular Formula: C24H28N4O3
• Molecular Weight: 420.50
• Purity: ≥95%
• Synonyms: 2-[4-[4-(4-amino-7,7-dimethylpyrimido[4,5-b][1,4]oxazin-6-yl)phenyl]-1-bicyclo[2.2.2]octanyl]acetic acid
• InChI: InChI=1S/C24H28N4O3/c1-22(2)19(28-18-20(25)26-14-27-21(18)31-22)15-3-5-16(6-4-15)24-10-7-23(8-11-24,9-12-24)13-17(29)30/h3-6,14H,7-13H2,1-2H3,(H,29,30)(H2,25,26,27)
• InChIKey: VGPKUACRBMPJLF-UHFFFAOYSA-N
• SMILES: CC1(C(=NC2=C(N=CN=C2O1)N)C3=CC=C(C=C3)C45CCC(CC4)(CC5)CC(=O)O)C

DGAT-1 inhibitor 2 is an effective inhibitor of DGAT-1;antiobesity agents.
IC50 value:
Target: DGAT-1
Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) is one of two known DGAT enzymes that catalyze the final step in triglyceride synthesis. Findings from genetically modified mice as well as pharmacological studies suggest that inhibition of DGAT1 is a promising strategy for the treatment of obesity and type 2 diabetes.

Reference

[1]. Matsuda D, Tomoda H. DGAT inhibitors for obesity. Curr Opin Investig Drugs. 2007 Oct;8(10):836-41.
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[2]. Birch, Alan M.; Birtles, Susan; Buckett, Linda K. et al. Discovery of a Potent, Selective, and Orally Efficacious Pyrimidinooxazinyl Bicyclooctaneacetic Acid Diacylglycerol Acyltransferase-1 Inhibitor. Journal of Medicinal Chemistry (2009), 52(6), 1558-15
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[3]. King AJ, Judd AS, Souers AJ. Inhibitors of diacylglycerol acyltransferase: a review of 2008 patents. Expert Opin Ther Pat. 2010 Jan;20(1):19-29.
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[4]. Cao J, Zhou Y, Peng H et al. Targeting Acyl-CoA:diacylglycerol acyltransferase 1 (DGAT1) with small molecule inhibitors for the treatment of metabolic diseases. J Biol Chem. 2011 Dec 2;286(48):41838-51.
 [Content Brief]