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

Pradigastat  (Synonyms: LCQ-908)

製品番号: HY-16278 純度: 98.88%
COA 取扱説明書 Technical Support

Pradigastat (LCQ-908) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC50 at 0.157 µM. 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. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro.

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Pradigastat 構造式

Pradigastat 構造式

CAS 番号 : 956136-95-1

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 264 在庫あり
Solution
10 mM * 1 mL in DMSO USD 264 在庫あり
Solid
5 mg USD 240 在庫あり
10 mg USD 370 在庫あり
50 mg USD 900 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 2 publication(s) in Google Scholar

Other Forms of Pradigastat:

Pradigastat 関連抗体

Top Publications Citing Use of Products

Acyltransferase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
ACAT1 ACAT2 MGAT2 ACAT

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

Pradigastat (LCQ-908) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC50 at 0.157 µM. 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. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro[1][2][3][4].

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]
Cellular Effect
Cell Line Type Value Description References
C2C12 EC50
71 nM
Compound: 1
Inhibition of DGAT1 in mouse C2C12 cells assessed as reduction in intracellular triglyceride production incubated for 2 hrs in presence of BSA-complexed oleate by LC/MS/MS analysis
Inhibition of DGAT1 in mouse C2C12 cells assessed as reduction in intracellular triglyceride production incubated for 2 hrs in presence of BSA-complexed oleate by LC/MS/MS analysis
[PMID: 31413796]
Sf9 IC50
55 nM
Compound: 1
Inhibition of recombinant human his-tagged DGAT1 expressed in Sf9 insect cells using oleoyl-CoA and diolein as substrates incubated for 30 mins by LC/MS/MS analysis
Inhibition of recombinant human his-tagged DGAT1 expressed in Sf9 insect cells using oleoyl-CoA and diolein as substrates incubated for 30 mins by LC/MS/MS analysis
[PMID: 31413796]
体外実験

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].
Pradigastat (2-20 μM; 8 h) inhibits the replication and production of hepatitis C virus in vitro[3].

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

Pradigastat 関連抗体
臨床実験
分子量

455.47

Synonyms

LCQ-908

分子式

C25H24F3N3O2
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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
10 mM 0.2196 mL 1.0978 mL 2.1955 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
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Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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    90% (20% SBE-β-CD in 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
純度とドキュメンテーション

純度: 98.88%

COA (244 KB) LCMS (96 KB)

取扱説明書 (2659 KB)
参考文献

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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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 908AcyltransferaseBCRPOATDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseBreast cancer resistance proteinABCG2Organic anion transporterDGAT1anti-obesityanti-diabeticOATPOAT3chylomicronstriglycerideInhibitorinhibitorinhibit

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