2. Metabolic Enzyme/Protease Membrane Transporter/Ion Channel
  3. Acyltransferase BCRP
  4. Pradigastat

Pradigastat  (Synonyms: LCQ-908)

Cat. No.: HY-16278 Purity: 98.88%
COA Handling Instructions

Molarity Calculator

Pradigastat (LCQ-908) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC50 of 5 µM, 1.66µM, 3.34µM and 0.973µM, respectively.

For research use only. We do not sell to patients.

Pradigastat Chemical Structure

Pradigastat Chemical Structure

CAS No. : 956136-95-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 264 In-stock
Solution
10 mM * 1 mL in DMSO USD 264 In-stock
Solid
5 mg USD 240 In-stock
10 mg USD 370 In-stock
50 mg USD 900 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Pradigastat:

Pradigastat Related Antibodies

Top Publications Citing Use of Products

View All Acyltransferase Isoform Specific Products:

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ACAT1 ACAT2 MGAT2 ACAT

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Pradigastat (LCQ-908) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC50 of 5 µM, 1.66µM, 3.34µM and 0.973µM, respectively.

IC50 & Target

Diacylglycerol acyltransferase 1 (DGAT1)[1]
IC50: 5 µM (BCRP); IC50: 1.66 µM (OATP1B1); IC50: 3.34 µM (OATP1B3); IC50: 0.973 µM (OAT3)[2]
In Vitro

Pradigastat (0-50 μM; 1 h) inhibits BCRP-mediated efflux activity in a dose-dependent manner in overexpressing human ovarian cancer cell lines with an IC50 of 5 µM[2].
Pradigastat (0-50 μM; 5 minutes) inhibits OATP1B1, OATP1B3, and OAT3 activities in a concentration-dependent manner with IC50 of 1.66µM, 3.34µM and 0.973µM, respectively[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pradigastat Related Antibodies
Clinical Trial
Molecular Weight

455.47

Formula

C25H24F3N3O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(O)C[C@H]1CC[C@H](C2=CC=C(C3=NC=C(NC4=CC=C(C(F)(F)F)N=C4)C=C3)C=C2)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (137.22 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1955 mL 10.9777 mL 21.9553 mL
5 mM 0.4391 mL 2.1955 mL 4.3911 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (5.49 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (5.49 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.88%

COA (244 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1955 mL 10.9777 mL 21.9553 mL 54.8884 mL
5 mM 0.4391 mL 2.1955 mL 4.3911 mL 10.9777 mL
10 mM 0.2196 mL 1.0978 mL 2.1955 mL 5.4888 mL
15 mM 0.1464 mL 0.7318 mL 1.4637 mL 3.6592 mL
20 mM 0.1098 mL 0.5489 mL 1.0978 mL 2.7444 mL
25 mM 0.0878 mL 0.4391 mL 0.8782 mL 2.1955 mL
30 mM 0.0732 mL 0.3659 mL 0.7318 mL 1.8296 mL
40 mM 0.0549 mL 0.2744 mL 0.5489 mL 1.3722 mL
50 mM 0.0439 mL 0.2196 mL 0.4391 mL 1.0978 mL
60 mM 0.0366 mL 0.1830 mL 0.3659 mL 0.9148 mL
80 mM 0.0274 mL 0.1372 mL 0.2744 mL 0.6861 mL
100 mM 0.0220 mL 0.1098 mL 0.2196 mL 0.5489 mL
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Pradigastat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pradigastat956136-95-1LCQ-908LCQ908LCQ 908AcyltransferaseBCRPDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseBreast cancer resistance proteinABCG2DGAT1anti-obesityanti-diabeticOATPOAT3chylomicronstriglycerideInhibitorinhibitorinhibit

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