| Description | Pradigastat (LCQ-908) is an orally active, potent and selective diacylglycerol acyltransferase 1 (DGAT1) inhibitor for the treatment of constipation, which may be used in the study of obesity and diabetes. |
| In vitro | Pradigastat 在 BCRP 过表达的人卵巢癌细胞系中以剂量依赖性方式抑制 BCRP 介导的外排活性，IC50 值为 5 μM。同样，pradigastat 以浓度依赖性方式抑制 OATP1B1、OATP1B3(雌二醇 17β 葡糖苷酸转运)和 OAT3(硫酸雌酮 3 转运)活性，估计 IC50 值分别为 1.66 ± 0.95 μM、3.34 ± 0.64 μM 和 0.973 ± 0.11 μM[3]。 |
| In vivo | 研究表明Pradigastat (LCQ-908) 能够抑制大鼠、狗和猴子的餐后甘油三酯水平。在脂蛋白脂肪酶(LPL)活性消除的大鼠中，Pradigastat可减少餐后血浆甘油三酯的积累。同时Pradigastat 能够降低餐后乳糜微粒甘油三酯 (CM-TG) 分泌到淋巴管的速率并减小乳糜微粒的大小[2]。 |
| Target activity | bovine 5-HT1D:6.6 (pKi), Rat hippocampus 5-HT1A receptor:6.3 (pKi), H1:6.5 (Rat, pKi), rat 5-HT2A:6.5 (pKi), Ca2+ channel:5.6 (Rat, pKi), Histamine H2:6.6 (guinea-pig, pKi) |
| Synonyms | ANJ908, LCQ908-NXA, LCQ908A, LCQ-908 |
| molecular weight | 455.47 |
| Molecular formula | C25H24F3N3O2 |
| CAS | 956136-95-1 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: <0.1 mg/mL (Insoluble) DMSO: 50 mg/mL (109.78 mM), Sonication is recommended. |
| References | 1. Meyers CD, et al. Effect of the DGAT1 inhibitor pradigastat on triglyceride and apoB48 levels in patients with familial chylomicronemia syndrome. Lipids Health Dis. 2015 Feb 18;14:8. 2. Charles DanielMeyersMD, et al. The DGAT1 inhibitor pradigastat decreases chylomicron secretion and prevents postprandial triglyceride elevation in humans. Journal of Clinical Lipidology. Volume 7, Issue 3, May-June 2013, Page 285. 3. Kulmatycki K, et al. Evaluation of a potential transporter-mediated drug interaction between ZD 4522 and pradigastat, a novel DGAT-1 inhibitor. Int J Clin Pharmacol Ther. 2015 May;53(5):345-55. |