Pradigastat

Pradigastat (LCQ-908) 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].

Product Specifications

CAS Number

[956136-95-1]

Product Name Alternative

LCQ-908

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Acyltransferase; BCRP; OAT

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Infection; Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/LCQ-908.html

Purity

99.59

Solubility

DMSO : 62.5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(O)C[C@H]1CC[C@H](C2=CC=C(C3=NC=C(NC4=CC=C(C(F)(F)F)N=C4)C=C3)C=C2)CC1

Molecular Formula

C25H24F3N3O2

Molecular Weight

455.47

Precautions

H302, H315, H319, H335

References & Citations

[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]Kulmatycki K, et al. 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.|[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.|[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.