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Pradigastat

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Purity:95.21%

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COA LCMS

Pradigastat

Catalog No. T11827Cas 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.

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Pack Size	Price	Availability
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

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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	H1:6.5 (Rat, pKi), Histamine H2:6.6 (guinea-pig, pKi), Rat hippocampus 5-HT1A receptor:6.3 (pKi), bovine 5-HT1D:6.6 (pKi), Ca2+ channel:5.6 (Rat, pKi), rat 5-HT2A:6.5 (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	ANJ908, LCQ908-NXA, LCQ908A, LCQ-908

Chemical Properties

Molecular Weight	455.47
Formula	C25H24F3N3O2
Cas No.	956136-95-1

Storage & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	2.1955 mL	10.9777 mL	21.9553 mL	109.7767 mL
5 mM	0.4391 mL	2.1955 mL	4.3911 mL	21.9553 mL
10 mM	0.2196 mL	1.0978 mL	2.1955 mL	10.9777 mL
20 mM	0.1098 mL	0.5489 mL	1.0978 mL	5.4888 mL
50 mM	0.0439 mL	0.2196 mL	0.4391 mL	2.1955 mL
100 mM	0.0220 mL	0.1098 mL	0.2196 mL	1.0978 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 mother liquor preparation method and in vivo formula preparation method:

For 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 DMSO TargetMol | 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 DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc