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Pradigastat

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Catalog No. T11827Cas No. 956136-95-1
Alias LCQ908-NXA, LCQ908A, LCQ-908, ANJ908

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

Pradigastat

😃Good
Purity: 95.21%
Catalog No. T11827Alias LCQ908-NXA, LCQ908A, LCQ-908, ANJ908Cas No. 956136-95-1
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 SizePriceAvailabilityQuantity
1 mg$113In Stock
2 mg$1635 days
5 mg$283In Stock
1 mL x 10 mM (in DMSO)$2975 days
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Purity:95.21%
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Product Introduction

Bioactivity
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].
AliasLCQ908-NXA, LCQ908A, LCQ-908, ANJ908
Chemical Properties
Molecular Weight455.47
FormulaC25H24F3N3O2
Cas No.956136-95-1
SmilesOC(=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 & Solubility Information
Storagestore 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
1mg5mg10mg50mg
1 mM2.1955 mL10.9777 mL21.9553 mL109.7767 mL
5 mM0.4391 mL2.1955 mL4.3911 mL21.9553 mL
10 mM0.2196 mL1.0978 mL2.1955 mL10.9777 mL
20 mM0.1098 mL0.5489 mL1.0978 mL5.4888 mL
50 mM0.0439 mL0.2196 mL0.4391 mL2.1955 mL
100 mM0.0220 mL0.1098 mL0.2196 mL1.0978 mL

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TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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