Pradigastat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Pradigastat (LCQ-908) 是一种有效的，选择性的，口服活性的二酰基甘油酰基转移酶 1 (DGAT1) 抑制剂。Pradigastat 具有抗肥胖和抗糖尿病作用。

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 中的溶解度 : 62.5 mg/mL (137.22 mM; 超声助溶 (<60°C)；H2O 中的溶解度 : < 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