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DGAT-1 inhibitor 2

Names

[ CAS No. ]:
942999-61-3

[ Name ]:
DGAT-1 inhibitor 2

[Synonym ]:
DGAT-1 inhibitor 2||Bicyclo[2.2.2]octane-1-acetic acid,4-[4-(4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1,4]oxazin-6-yl)phenyl]
DGAT-1 inhibitor 2
bicyclo[2.2.2]octane-pyrimido[4,5-b][1,4]oxazine deriv.,4
Bicyclo[2.2.2]octane-1-acetic acid,4-[4-(4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1,4]oxazin-6-yl)phenyl]
CS-0982

Biological Activity

[Description]:

DGAT-1 inhibitor 2 is an effective inhibitor of DGAT-1;antiobesity agents.IC50 value:Target: DGAT-1Acyl-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.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Acyltransferase
Research Areas >> Metabolic Disease

[References]

[1]. Matsuda D, Tomoda H. DGAT inhibitors for obesity. Curr Opin Investig Drugs. 2007 Oct;8(10):836-41.

[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

[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.

[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.


[Related Small Molecules]

Avasimibe | LCQ-908 | DGAT-3 | A922500 | Xanthohumol | PF-04620110 | AZD7687 | MGAT2-IN-1 | DGAT1-IN-1 | K-604 dihydrochloride | PF-06471553 | YM17E | ABT-046 | RP 70676 | Furan-2-carboxylic acid

Chemical & Physical Properties

[ Molecular Formula ]:
C24H28N4O3

[ Molecular Weight ]:
420.50400

[ Exact Mass ]:
420.21600

[ PSA ]:
110.69000

[ LogP ]:
4.43410

[ Storage condition ]:
2-8℃

Related Compounds

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