Pradigastat sodium  (Synonyms: LCQ 908 sodium)

Pradigastat sodium (LCQ 908 sodium) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC₅₀ at 0.157 µM. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC₅₀ of 5 µM, 1.66µM, 3.34µM and 0.973µM, respectively. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro^[1][2][3][4].

Diacylglycerol acyltransferase 1 (DGAT1)^[1]
IC₅₀: 5 µM (BCRP); IC₅₀: 1.66 µM (OATP1B1); IC₅₀: 3.34 µM (OATP1B3); IC₅₀: 0.973 µM (OAT3)^[2]

Pradigastat (0-50 μM; 1 小时) 在过表达 BCRP 的人卵巢癌细胞系中以剂量依赖性的方式抑制 BCRP 介导的外排活性， IC₅₀ 为 5 µM^[2]。
Pradigastat (0-50 μM; 5 分钟) 以浓度依赖性的方式抑制 OATP1B1、OATP1B3 和 OAT3 活性，IC₅₀ 分别为 1.66 µM、3.34µM 和 0.973 µM^[2]。
Pradigastat (2-20 μM；8 小时) 在体外可以抑制丙型肝炎病毒的复制和产生^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

477.45

C₂₅H₂₃F₃N₃NaO₂

956136-98-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [2]. 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.  [Content Brief]

  [3]. Gane E, et al. A Diacylglycerol Transferase 1 Inhibitor Is a Potent Hepatitis C Antiviral in Vitro but Not in Patients in a Randomized Clinical Trial. ACS Infect Dis. 2017 Feb 10;3(2):144-151.  [Content Brief]

  [4]. Hong DJ, et al. Synthesis and biological evaluation of novel thienopyrimidine derivatives as diacylglycerol acyltransferase 1 (DGAT-1) inhibitors. J Enzyme Inhib Med Chem. 2020 Dec;35(1):227-234.  [Content Brief]