Pradigastat

• CAT Number: I005662
• CAS Number: 956136-95-1
• Molecular Formula: C25H24F3N3O2
• Molecular Weight: 455.47
• Purity: ≥95%
• Synonyms: 2-[4-[4-[5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl]phenyl]cyclohexyl]acetic acid
• InChI: InChI=1S/C25H24F3N3O2/c26-25(27,28)23-12-10-21(15-30-23)31-20-9-11-22(29-14-20)19-7-5-18(6-8-19)17-3-1-16(2-4-17)13-24(32)33/h5-12,14-17,31H,1-4,13H2,(H,32,33)
• InChIKey: GXALXAKNHIROPE-UHFFFAOYSA-N
• SMILES: C1CC(CCC1CC(=O)O)C2=CC=C(C=C2)C3=NC=C(C=C3)NC4=CN=C(C=C4)C(F)(F)F

Pradigastat (LCQ-908) is a potent, selective and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor. Pradigastat has anti-obesity and anti-diabetic effects[1][2].
Pradigastat inhibits breast cancer resistance protein (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. Pradigastat inhibits OATP1B1, OATP1B3, and OAT3 activity in a concentration-dependent manner with estimated IC50 values of 1.66 μM, 3.34 μM, and 0.973 μM, respectively[2].
Pradigastat (LCQ-908) inhibits the postprandial triglyceride levels in rats, dogs and monkeys. In rats whose lipoprotein lipase (LPL) activity has been abolished, Pradigastat reduces the postprandial accumulation of plasma triglyceride. Pradigastat decreases the postprandial rate of chylomicron triglyceride (CM-TG) secretion into the lymphatic duct and reduces the size of chylomicrons[3].

Reference

[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.
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[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]. 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.