LCQ-908DGAT1 inhibitor CAS# 956136-95-1 |
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Quality Control & MSDS
3D structure
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Number of papers citing our products
| Cas No. | 956136-95-1 | SDF | Download SDF |
| PubChem ID | 53387035 | Appearance | Powder |
| Formula | C25H24F3N3O2 | M.Wt | 455.47 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Pradigastat | ||
| Solubility | DMSO : 16.67 mg/mL (36.60 mM; ultrasonic and warming and heat to 60°C) H2O : < 0.1 mg/mL (insoluble) H2O : < 0.1 mg/mL (insoluble) | ||
| Chemical Name | 2-[4-[4-[5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl]phenyl]cyclohexyl]acetic acid | ||
| SMILES | C1CC(CCC1CC(=O)O)C2=CC=C(C=C2)C3=NC=C(C=C3)NC4=CN=C(C=C4)C(F)(F)F | ||
| Standard InChIKey | GXALXAKNHIROPE-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C25H24F3N3O2/c26-25(27,28)23-12-10-21(15-30-23)31-20-9-11-22(29-14-20)19-7-5-18(6-8-19)17-3-1-16(2-4-17)13-24(32)33/h5-12,14-17,31H,1-4,13H2,(H,32,33) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | LCQ-908 is a new generation of diacylglycerol acyltransferase 1 (DGAT1) inhibitor as anti-obesity and anti-diabetic agents.In Vivo:LCQ-908 is a potent inhibitor of DGAT1, and has been used for the phase II clinical trials to treat diabetes and obesity[1]. References: | |||||
LCQ-908 Dilution Calculator
LCQ-908 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.1955 mL | 10.9777 mL | 21.9553 mL | 43.9107 mL | 54.8884 mL |
| 5 mM | 0.4391 mL | 2.1955 mL | 4.3911 mL | 8.7821 mL | 10.9777 mL |
| 10 mM | 0.2196 mL | 1.0978 mL | 2.1955 mL | 4.3911 mL | 5.4888 mL |
| 50 mM | 0.0439 mL | 0.2196 mL | 0.4391 mL | 0.8782 mL | 1.0978 mL |
| 100 mM | 0.022 mL | 0.1098 mL | 0.2196 mL | 0.4391 mL | 0.5489 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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DGAT1 inhibitors as anti-obesity and anti-diabetic agents.[Pubmed:20597032]
Curr Opin Drug Discov Devel. 2010 Jul;13(4):489-96.
Since 2008, significant advances have been made in understanding the role of diacylglycerol acyl transferase-1 (DGAT1) in disease states such as diabetes and obesity. Gene deletion and overexpression studies have provided important new insights into the function of DGAT1, as have the first reports from preclinical models of small-molecule inhibitor effects, which are discussed in this review in relation to the phenotypes of DGAT knockout and overexpression models. The progress of medicinal chemistry efforts has resulted in a new generation of DGAT1 inhibitors that have progressed into clinical development, with the leading compound LCQ-908 (Novartis AG) now in phase II clinical trials. This exciting progress has led researchers to anticipate that an understanding of the human pharmacology of DGAT1 inhibitors, as well as their potential as therapeutic agents for the treatment of diabetes and obesity, will be achieved in the next few years.
