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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.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $84 | - | In Stock |
| Description | 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. |
| Targets&IC50 | Histamine H2:6.6 (guinea-pig, pKi), 5-HT2A (rat):6.5 (pKi), bovine 5-HT1D:6.6 (pKi), Ca2+ channel:5.6 (Rat, pKi), H1:6.5 (Rat, pKi), Rat hippocampus 5-HT1A receptor:6.3 (pKi) |
| In vitro | Pradigastat inhibits BCRP-mediated efflux activity in BCRP-overexpressing human ovarian cancer cell lines in a dose-dependent manner, with an IC50 value of 5 μM. Similarly, pradigastat demonstrates concentration-dependent inhibition of OATP1B1, OATP1B3 (estradiol 17β-glucuronide transport), and OAT3 (sulfated estrone-3-sulfate transport), with estimated IC50 values of 1.66 ± 0.95 μM, 3.34 ± 0.64 μM, and 0.973 ± 0.11 μM, respectively.3]. |
| In vivo | Research indicates that Pradigastat (LCQ-908) can inhibit postprandial triglyceride levels in rats, dogs, and monkeys. In rats with eliminated lipoprotein lipase (LPL) activity, Pradigastat reduces postprandial plasma triglyceride accumulation. Additionally, Pradigastat lowers the rate of postprandial chylomicron triglyceride (CM-TG) secretion into the lymphatic system and decreases chylomicron particle size[2]. |
| Synonyms | LCQ908-NXA, LCQ908A, LCQ-908, ANJ908 |
| Molecular Weight | 455.47 |
| Formula | C25H24F3N3O2 |
| Cas No. | 956136-95-1 |
| Smiles | OC(=O)C[C@H]1CC[C@@H](CC1)c1ccc(cc1)-c1ccc(Nc2ccc(nc2)C(F)(F)F)cn1 |
| Relative Density. | 1.286 g/cm3 (Predicted) |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: <0.1 mg/mL (Insoluble) DMSO: 50 mg/mL (109.78 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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