產(chǎn)品目錄

規(guī)格	10 mM * 1 mL in DMSO 5mg 10mg 50mg
CAS	956136-95-1
別名	Pradigastat;LCQ908;LCQ 908
化學(xué)名	2-[4-[4-[5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl]phenyl]cyclohexyl]acetic acid
分子式	C25H24F3N3O2
分子量	455.47
溶解度	Soluble in DMSO
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)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.

特別提醒：

1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請(qǐng)穿好實(shí)驗(yàn)服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

在線咨詢

留言注意事項(xiàng)：

1.遵守中華人民共和國(guó)有關(guān)法律、法規(guī)，尊重網(wǎng)上道德，承擔(dān)一切因您的行為而直接或間接引起的法律責(zé)任。

2.請(qǐng)您真實(shí)的反映產(chǎn)品的情況,不要捏造、誣蔑、造謠。如對(duì)產(chǎn)品有任何疑問(wèn),也可以留言咨詢。

3.未經(jīng)本站同意，任何人不得利用本留言簿發(fā)布個(gè)人或團(tuán)體的具有廣告性質(zhì)的信息或類似言論。

您感興趣的產(chǎn)品*
您的單位*
聯(lián)系人*
聯(lián)系電話*
詳細(xì)地址*
常用郵箱*
請(qǐng)輸入您對(duì)我們的意見(jiàn)或建議*
驗(yàn)證碼*