An orally, bioavailable human and mouse diacylglycerol acyltransferase DGAT-1 inhibitor (IC50 = 9nM and 22 nM, respectively), which may target DGAT-2 (IC50 = 53 uM) and the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 (IC50 = 296 uM) with equal or less potencies. In vivo activities indicate an effective reduction in serum triglycerides, FFA concentrations, and total cholesterol by 53%, 55% and 25%, respectively, compared to baseline, when administered orally at 3 mg/kg daily dosages in Dyslipidemic Hamsters. Similar reductions in triglyceride and FFA concentrations were shown in Zucker fatty rats.

June 21, 2017

prudect name : An orally, bioavailable human and mouse diacylglycerol acyltransferase DGAT-1 inhibitor (IC50 = 9nM and 22 nM, respectively), which may target DGAT-2 (IC50 = 53 uM) and the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 (IC50 = 296 uM) with equal or less potencies. In vivo activities indicate an effective reduction in serum triglycerides, FFA concentrations, and total cholesterol by 53%, 55% and 25%, respectively, compared to baseline, when administered orally at 3 mg/kg daily dosages in Dyslipidemic Hamsters. Similar reductions in triglyceride and FFA concentrations were shown in Zucker fatty rats.
A 922500

Synonyms: A 922500CAS NO: 959122-11-3Molecular Formula: C₂₆H₂₄N₂O₄Molecular Weight: 428.48Purity: 98% minSolubility: In DMSOStorage: −20°C

379231-04-6 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18496845