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CAS No.: 956136-95-1

Pradigastat Catalog No. CSN16959

Synonyms: LCQ-908

LCQ-908 is a potent and oral active diacylglycerol acyltransferase 1 (DGAT1) inhibitor, used as anti-obesity and anti-diabetic agents.

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实验方案

技术信息

生物活性

描述LCQ-908 is a potent and oral active diacylglycerol acyltransferase 1 (DGAT1) inhibitor, used as anti-obesity and anti-diabetic agents. DGAT-1 is recognized to catalyze the conversion of diacylglycerol and fatty acyl CoA to triacylglycerol, which is highly expressed in the small intestine and plays a key role in postprandial triglyceride synthesis. LCQ908 inhibited BCRP-mediated efflux activity in a dose-dependent fashion in a BCRP over-expressing human ovarian cancer cell line with an IC50 value of 5 μM^[3]. LCQ908 inhibited OATP1B1, OATP1B3 (estradiol 17β glucuronide transport), and OAT3 (estrone 3 sulfate transport) 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^[3]. LCQ908 was fond to suppress the postprandial triglyceride levels in rats, dogs as well as monkeys. LCQ908 decreased the postprandial rate of CM-TG secretion into the lymphatic duct and reduced the size of CMs^[1]. In a clinical trial, LCQ908 was absorbed slowly, with a median tmax of ∼10 hours and eliminated slowly with a long half-life^[4]. LCQ908 treatment led to dose-dependent suppression of postprandial triglyceride excursions over 9 hours following a high-fat meal test. In addition, LCQ908 suppressed postprandial glucose and insulin and increased plasma glucagon-like peptide-1 levels^[4].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00901979	Type 2 Diabetes Mellitus	Phase 2	Completed	-	-
NCT01594983	Non Familial Chylocmicronemia ... more >>Syndrome (Non-FCS) Collapse <<	Phase 2	Completed	-	-
NCT01387958	Hepatitis C	Phase 2	Terminated(Terminated early du... more >>e to futility) Collapse <<	-	New Zealand ... more >> Novartis Investigative Site Auckland, New Zealand Novartis Investigative Site Christchurch, New Zealand Collapse <<

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参考文献

[1] Jian Z, Ray T, et al. Proton exchange reactions in isotope chemistry (II) synthesis of stable isotope-labeled LCQ908. J Labelled Comp Radiopharm. 2014 Oct;57(12):670-3.
[2] Bauer D, Soon RL, et al. The DGAT1 inhibitor pradigastat does not induce photosensitivity in healthy human subjects: a randomized controlled trial using three defined sunlight exposure conditions. Photochem Photobiol Sci. 2016 Aug 31;15(9):1155-1162.
[3] Kulmatycki K, Hanna I, Meyers D, Salunke A, Movva A, Majumdar T, Natrillo A, Vapurcuyan A, Rebello S, Sunkara G, Chen J. Evaluation 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. doi: 10.5414/CP202275. PMID: 25740267.
[4] Meyers CD, Amer A, Majumdar T, Chen J. Pharmacokinetics, pharmacodynamics, safety, and tolerability of pradigastat, a novel diacylglycerol acyltransferase 1 inhibitor in overweight or obese, but otherwise healthy human subjects. J Clin Pharmacol. 2015 Sep;55(9):1031-41. doi: 10.1002/jcph.509. Epub 2015 May 27. PMID: 25854859.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1955 mL
- 10.9776 mL
- 21.9552 mL
- 5 mM
- 0.4391 mL
- 2.1955 mL
- 4.3910 mL
- 10 mM
- 0.2196 mL
- 1.0978 mL
- 2.1955 mL

技术信息

CAS号

956136-95-1

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H24F3N3O2

运输

蓝冰

分子量

455.47

别名

LCQ-908

溶解度

DMSO	16.67 mg/mL (36.6 mM)
Water	Insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00901979	Type 2 Diabetes Mellitus	Phase 2	Completed	-	-
NCT01594983	Non Familial Chylocmicronemia ... more >>Syndrome (Non-FCS) Collapse <<	Phase 2	Completed	-	-
NCT01387958	Hepatitis C	Phase 2	Terminated(Terminated early du... more >>e to futility) Collapse <<	-	New Zealand ... more >> Novartis Investigative Site Auckland, New Zealand Novartis Investigative Site Christchurch, New Zealand Collapse <<
NCT01146522	Hyperlipoproteinemia	Phase 1 Phase 2	Completed	-	Canada ... more >> Novartis Investigative Site Quebec, Canada Collapse <<
NCT01811472	Non-alcoholic Fatty Liver Dise... more >>ase (NAFLD) Collapse <<	Phase 2	Completed	-	United States, Alabama ... more >> Novartis Investigative Site Mobile, Alabama, United States, 36608 United States, California Novartis Investigative Site San Diego, California, United States, 92114 United States, Florida Novartis Investigative Site Gainesville, Florida, United States, 32610-0277 Novartis Investigative Site Miami, Florida, United States, 33126 Novartis Investigative Site Tamarac, Florida, United States, 33319 United States, Hawaii Novartis Investigative Site Honolulu, Hawaii, United States, 96814 United States, Kentucky Novartis Investigative Site Louisville, Kentucky, United States, 40213 United States, Mississippi Novartis Investigative Site Tupelo, Mississippi, United States, 38801 United States, Texas Novartis Investigative Site Houston, Texas, United States, 77030 Novartis Investigative Site Plano, Texas, United States, 75093 United States, Virginia Novartis Investigative Site Richmond, Virginia, United States, 23298 Collapse <<
NCT01589237	Familial Chylomicronemia Syndr... more >>ome (FCS) (HLP Type I) Collapse <<	Phase 3	Terminated(Interim analysis su... more >>ggested that size of benefit anticipated from continued participation of patients in Part B no longer supported trial extension beyond Part A) Collapse <<	-	United States, Washington ... more >> Novartis Investigative Site Seatlle, Washington, United States, 98104 Canada, Quebec Novartis Investigative Site Chicoutimi, Quebec, Canada, G7H 7P2 Novartis Investigative Site Ste-Foy, Quebec, Canada, G1V4M6 Canada Novartis Investigative Site Ouest-Montreal, Canada, H2W1R7 France Novartis Investigative Site Nantes, France, 44093 Novartis Investigative Site Paris Cedex 13, France, 75651 Germany Novartis Investigative Site Hamburg, Germany, 20246 Netherlands Novartis Investigative Site Meibergdreef 9, Netherlands, 1105 AZ South Africa Novartis Investigative Site Cape Town, South Africa, 7925 United Kingdom Novartis Investigative Site Manchester, United Kingdom, M13 9NT Collapse <<
NCT01811472	-	-	Completed	-	-
NCT01474434	Coronary Artery Disease ... more >> Hypertriglyceridemia Collapse <<	Phase 2	Terminated(The study was termi... more >>nated based on interim analysis. See detailed description.) Collapse <<	-	United States, California ... more >> Novartis Investigative Site Pasadena, California, United States, 91105 Collapse <<
NCT01594957	Hepatic Impairment	Phase 1	Completed	-	United States, Florida ... more >> Novartis Investigative Site Miami, Florida, United States, 33136 Novartis Investigative Site Orlando, Florida, United States, 32809 Collapse <<
NCT01589237	-	-	Terminated(Interim analysis su... more >>ggested that size of benefit anticipated from continued participation of patients in Part B no longer supported trial extension beyond Part A) Collapse <<	-	-
NCT01514461	Familial Chylomicronemia Syndr... more >>ome (FCS) Collapse <<	Phase 3	Completed	-	United States, Washington ... more >> Novartis Investigative Site Seatlle, Washington, United States, 98104 Canada, Quebec Novartis Investigative Site Chicoutimi, Quebec, Canada, G7H 7P2 Novartis Investigative Site Ste-Foy, Quebec, Canada, G1V4M6 Canada Novartis Investigative Site Ouest-Montreal, Canada, H2W1R7 France Novartis Investigative Site Bron, France, 69677 Novartis Investigative Site Nantes, France, 44093 Novartis Investigative Site Paris Cedex 13, France, 75651 Germany Novartis Investigative Site Hamburg, Germany, 20246 Novartis Investigative Site Köln, Germany, 50937 Netherlands Novartis Investigative Site Meibergdreef 9, Netherlands, 1105 AZ South Africa Novartis Investigative Site Cape Town, South Africa, 7925 Spain Novartis Investigative Site Malaga, Andalucia, Spain, 29010 Novartis Investigative Site Sevilla, Andalucia, Spain, 41013 United Kingdom Novartis Investigative Site Manchester, United Kingdom, M13 9NT Collapse <<
NCT01474434	-	-	Terminated(The study was termi... more >>nated based on interim analysis. See detailed description.) Collapse <<	-	-
NCT01558323	Renal Impairment	Phase 1	Completed	-	United States, Florida ... more >> Novartis Investigative Site Orlando, Florida, United States, 32809 United States, Tennessee Novartis Investigative Site Knoxville, Tennessee, United States, 37920 Collapse <<
NCT01514461	-	-	Completed	-	-

Pradigastat Catalog No. CSN16959

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