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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

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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 SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$84-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:95.21%
Appearance:Solid
Color:Yellow
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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
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].
SynonymsLCQ908-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/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
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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent 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.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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Dose Conversion

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Tech Support

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Keywords

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