Discovery of PF-04620110, a potent, selective, and orally bioavailable inhibitor of DGAT-1

ACS Medicinal Chemistry Letters

Volumn 2, Issue 5, 2011, Pages 407-412

  Dow, Robert L ^a   Li, Jian Cheng ^a   Pence, Michael P ^a   Gibbs, E Michael ^a   Laperle, Jennifer L ^a   Litchfield, John ^a   Piotrowski, David W ^a   Munchhof, Michael J ^a   Manion, Tara B ^a   Zavadoski, William J ^a   Walker, Gregory S ^a   McPherson, R Kirk ^a   Tapley, Susan ^a   Sugarman, Eliot ^a   Guzman Perez, Angel ^a   Dasilva Jardine, Paul ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

acyl glucuronide; DGAT 1; diabetes; obesity; phototoxicity; triglyceride

Indexed keywords

ACYLTRANSFERASE INHIBITOR; CARBOXYLIC ACID; DIACYLGLYCEROL ACYLTRANSFERASE 1; LACTAM; PF 04620110; TRIACYLGLYCEROL; TRIETHYLAMINE; UNCLASSIFIED DRUG;

ACYLATION; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; DRUG BIOAVAILABILITY; DRUG HALF LIFE; DRUG INHIBITION; DRUG PENETRATION; DRUG POTENCY; DRUG SELECTIVITY; HYDROLYSIS; IC 50; IN VIVO STUDY; NONHUMAN; PLASMA CLEARANCE; PRIORITY JOURNAL; RAT; SYNTHESIS; TRIACYLGLYCEROL BLOOD LEVEL;

MUS; RODENTIA;

EID: 79956071958     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml200051p     Document Type: Article

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31. 0-4 h; data are included in Supporting Information. The free fraction of 3 in rat plasma is 0.09.
32. The human pharmacokinetic and pharmacodynamic predictions of 3 will be the subject of a separate report.