Pradigastat
Based on 2 publication(s) in Google Scholar
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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- Purity: 99.88%
- CAS No.: 956136-95-1
- 화학식: C25H24F3N3O2
- 분자량:455.47
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) Pradigastat
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Biological Activity
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]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| C2C12 | EC50 |
71 nM
Compound: 1
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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
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[PMID: 31413796] |
| Sf9 | IC50 |
55 nM
Compound: 1
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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
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[PMID: 31413796] |
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.
Chemical Information
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CAS No. 956136-95-1
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Appearance Solid
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분자량 455.47
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화학식 C25H24F3N3O2
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Color Light yellow to yellow
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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
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Synonyms
LCQ-908
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Neuron
2020 Jan 22;105(2):276-292.e5. PMID: 31786011 -
Curr Atheroscler Rep
Managing of Dyslipidaemia Characterized by Accumulation of Triglyceride-Rich Lipoproteins. [Abstract]2022 Jan;24(1):1-12. PMID: 35107764
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (272 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
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- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Meyers CD, et al. Effect of the DGAT1 inhibitor pradigastat on triglyceride and apoB48 levels in patients with familial chylomicronemia syndrome. Lipids Health Dis. 2015 Feb 18;14:8. [Content Brief]
[2]. Kulmatycki K, et al. Evaluation of a potential transporter-mediated drug interaction between rosuvastatin and pradigastat, a novel DGAT-1 inhibitor. Int J Clin Pharmacol Ther. 2015 May;53(5):345-55. [Content Brief]
[3]. Gane E, et al. A Diacylglycerol Transferase 1 Inhibitor Is a Potent Hepatitis C Antiviral in Vitro but Not in Patients in a Randomized Clinical Trial. ACS Infect Dis. 2017 Feb 10;3(2):144-151. [Content Brief]
[4]. Hong DJ, et al. Synthesis and biological evaluation of novel thienopyrimidine derivatives as diacylglycerol acyltransferase 1 (DGAT-1) inhibitors. J Enzyme Inhib Med Chem. 2020 Dec;35(1):227-234. [Content Brief]
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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