LCQ-908
(Synonyms: Pradigastat;LCQ908;LCQ 908) 目录号 : GC11036
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
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| Cas No. | 956136-95-1 | SDF | |
| 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 SMILES | C1CC(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°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1955 mL | 10.9777 mL | 21.9553 mL |
| 5 mM | 0.4391 mL | 2.1955 mL | 4.3911 mL |
| 10 mM | 0.2196 mL | 1.0978 mL | 2.1955 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。