Pradigastat

Research use only, not for human use.

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.

Pradigastat (LCQ-908) is a potent, selective and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor. Pradigastat has anti-obesity and anti-diabetic effects.

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.

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.

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Metabolic Enzyme/Protease

Transferase

Transferase

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956136-95-1

455.47

C25H24F3N3O2

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (137.22 mM; Ultrasonic (<60°C); H2O : < 0.1 mg/mL (insoluble)

OC(=O)C[C@H]1CC[C@@H](CC1)c1ccc(cc1)-c1ccc(Nc2ccc(nc2)C(F)(F)F)cn1

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(-20℃)

With Ice Pack

≥ 2 years