63405-90-3Relevant academic research and scientific papers
Intestinally targeted diacylglycerol acyltransferase 1 (DGAT1) inhibitors robustly suppress postprandial triglycerides
Serrano-Wu, Michael H.,Coppola, Gary M.,Gong, Yongjin,Neubert, Alan D.,Chatelain, Ricardo,Clairmont, Kevin B.,Commerford, Renee,Cosker, Theresa,Daniels, Thomas,Hou, Ying,Jain, Monish,Juedes, Marlene,Li, Lisha,Mullarkey, Tara,Rocheford, Erik,Sung, Moo Je,Tyler, Andrew,Yang, Qing,Yoon, Taeyoung,Hubbard, Brian K.
, p. 411 - 415 (2012/07/03)
High DGAT1 expression levels in the small intestine highlight the critical role this enzyme plays in nutrient absorption. Identification of inhibitors which predominantly inhibit DGAT1 in the gut is an attractive drug discovery strategy with anticipated benefits of reduced systemic toxicity. In this report we describe our discovery and optimization of DGAT1 inhibitors whose plasma exposure is minimized by the action of transporters, including the P-glycoprotein transporter. The impact of this unique absorption profile on efficacy in rat and dog efficacy models is presented.
OXADIAZOLE- AND OXAZOLE-SUBSTITUTED BENZIMIDAZOLE- AND INDOLE-DERIVATIVES AS DGAT1 INHIBITORS
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Page/Page column 103-104, (2009/05/29)
The present invention provides oxadiazolyl- substituted benzimidazole- and idole-derivates that are useful for treating conditions or disorders associated with DGAT1 activity in animals, particularly humans.
METHOD OF TREATMENT
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Page/Page column 65, (2008/12/06)
Method of of preventing or treating myocardial ischemia by inhibiting DGAT1 enzyme with a DGAT1 inhibitor compound.
