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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 | Availability | Quantity |
---|---|---|---|
1 mg | $113 | In Stock | |
2 mg | $163 | 5 days | |
5 mg | $283 | In Stock | |
1 mL x 10 mM (in DMSO) | $297 | 5 days |
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 | Rat hippocampus 5-HT1A receptor:6.3 (pKi), Histamine H2:6.6 (guinea-pig, pKi), rat 5-HT2A:6.5 (pKi), bovine 5-HT1D:6.6 (pKi), Ca2+ channel:5.6 (Rat, pKi), H1:6.5 (Rat, 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]. |
Alias | 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. | |||||||||||||||||||||||||||||||||||
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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