"目录号: HY-15197
Metabolic Enzyme/Protease-
ABT-046是高活性、口服生物相容性的二酰基甘油酰基转移酶1（DGAT-1）抑制剂，IC50为8 nM。
DGAT
相关产品
LCQ-908-A 922500-T863-PF-04620110-AZD7687-DGAT-1 inhibitor 2-Xanthohumol-DGAT1-IN-1-
生物活性
Description
ABT-046 is a potent, selective, and orally bioavailable Diacylglycerol acyltransferase 1 (DGAT-1 ) inhibitor (IC50= 8 nM).IC50 value: 8 nM [1]Target: DGAT-1Oral administration at doses ≥0.03 mg/kg significantly reduced postprandial triglycerides in mice following an oral lipid challenge. Further assessment in both acute and chronic safety pharmacology and toxicology studies demonstrated a clean profile up to high plasma levels, thus culminating in the nomination of 14 as clinical candidate ABT-046.
References
[1].Yeh VS, et al. Identification and preliminary characterization of a potent, safe, and orally efficacious inhibitor of Acyl-CoA: Diacylglycerol acyltransferase 1. J Med Chem. 2012 Feb 23;55(4):1751-1757.