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LCQ-908
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
LCQ-908图片
CAS NO:956136-95-1
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
LCQ-908 (LCQ-908) 是一种有效的、选择性的和具有口服活性的二酰基甘油酰基转移酶 1 (DGAT1) 抑制剂。
Cas No.956136-95-1
别名Pradigastat;LCQ908;LCQ 908
化学名2-[4-[4-[5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl]phenyl]cyclohexyl]acetic acid
Canonical SMILESC1CC(CCC1CC(=O)O)C2=CC=C(C=C2)C3=NC=C(C=C3)NC4=CN=C(C=C4)C(F)(F)F
分子式C25H24F3N3O2
分子量455.47
溶解度Soluble in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 5 μM for BCRP-mediated efflux activity

LCQ908 is a diacylglycerol acyltransferase-1 (DGAT-1) inhibitor. DGAT-1 has been recognized to catalyze the final committed step of processing dietary fatty acids into triglycerides carried on chylomicrons for transport around the body. Thus,inhibition of DGAT-1 represents a novel approach to treat metabolic disease.

In vitro: In vitro studies suggest that glucuronidation is the predominant metabolism pathway for elimination of LCQ908 in humans. LCQ908 inhibited BCRP-mediated efflux activity in a dose-dependent fashion with an IC50 value of 5 μM. LCQ908 also inhibited OATP1B1, OATP1B3, and OAT3 activity in a concentration-dependent manner with estimated IC50 values of 1.66 ± 0.95 μM, 3.34 ± 0.64 μM, and 0.973 ± 0.11 μM, respectively [1].

In vivo: LCQ908 was fond to suppress the postprandial triglyceride levels in rats, dogs as well as monkeys. In rats whose LPL activity had been abolished, LCQ908 reduced the postprandial accumulation of plasma triglyceride. Additional, LCQ908 decreased the postprandial rate of CM-TG secretion into the lymphatic duct and reduced the size of CMs [2].

Clinical trial: In a clinical trial, LCQ908 was found to be able to lower fasting triglyceride levels in familial chylomicronemia syndrome patients maintained on a very low-fat diet, and represents a potential drug treatment for this orphan disease [3].

References:
[1] Kulmatycki K,Hanna I,Meyers D,Salunke A,Movva A,Majumdar T,Natrillo A,Vapurcuyan A,Rebello S,Sunkara G,Chen JEvaluation of a potential transporter-mediated drug interaction between rosuvastatin and pradigastat, a novel DGAT-1 inhibitor. Int J Clin Pharmacol Ther.2015 May;53(5):345-55.
[2] Meyers CD, Serrano-Wu M, Amer A, Chen J, Eric R, Commerford R, et al. The DGAT1 inhibitor pradigastat decreases chylomicron secretion and prevents postprandial triglyceride elevation in humans [abstract]J Clin Lipidol.2013;7:285.
[3] Charles Meyers, Daniel Gaudet, Karine Tremblay, Ahmed Amer, Jin Chen, Feng Aimin. The DGAT1 Inhibitor LCQ908 decreases triglyceride levels in patients with the familial chylomicronemia syndrome. Journal of Clinical Lipidology, Vol 6, No 3, June 2012, 266-267.