Leriglitazone
Based on 1 Customer Validation
Leriglitazone (MIN-102; Hydroxypioglitazone) is an orally active and a BBB-penetrable PPARγ agonist with an EC50 of 9 μM. Leriglitazone, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone can be used in the study of neuroinflammatory and neurodegenerative diseases.
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- Pureté : 99.09%
- CAS No.: 146062-44-4
- Formule: C19H20N2O4S
- Masse moléculaire:372.44
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[4]|
PPAR-γ 9 μM (EC50) |
In Vitro
Leriglitazone (100 nM; 45 days) increases PKAN astrocyte activity and respiratory activity, and reduces iron accumulation[1].
Leriglitazone (50-500 nM; 5 days) increases Frataxin levels, promots cell survival and improves neuronal degeneration and mitochondrial function in Frataxin-deficient DRG neurons[2].
Leriglitazone (0.5-2 μM; 7 days) prevents lipid droplet accumulation in frataxin-deficient cardiomyocytes[2].
Leriglitazone (100-500 nM; 48 h) regulates the expression of PPARγ signaling pathway related genes, increases mitochondrial function and reduces oxidative damage in Rett fibroblasts[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Frataxin-deficient DRG neurons
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Concentration:500 nM
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Incubation Time:5 days
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Result:Increased the level of frataxin.
In Vivo
Leriglitazone (75 mg/kg; Feed administration; 7 months) has an improved effect in Rett mouse model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:YG8sR mice[2]
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Dosage:50 mg/kg
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Administration:Feed administration; 8 months
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Result:Did not change the weight gain of YG8sR mice.
Improved the performance of the YG8sR mice in the case of the balance beam test.
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Animal Model:Rett female mice[3]
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Dosage:75 mg/kg
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Administration:Feed administration; 7 months
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Result:Corrected the defect of ATP concentration and lipid peroxidation in hippocampus and cerebellum.
Reduce the level of 8-OHdG, ROS, MnSOD and GPX.
Improved overall health and exploratory behavior in mice.
Chemical Information
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CAS No. 146062-44-4
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Appearance Solid
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Masse moléculaire 372.44
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Formule C19H20N2O4S
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Color White to light yellow
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SMILES
O=C(N1)SC(CC2=CC=C(OCCC3=NC=C(C(O)C)C=C3)C=C2)C1=O
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Synonyms
MIN-102; Hydroxypioglitazone
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 200 mg/mL (537.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (13.42 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (13.42 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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:
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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.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Santambrogio P, et al PPAR Gamma Agonist Leriglitazone Recovers Alterations Due to Pank2-Deficiency in hiPS-Derived Astrocytes. Pharmaceutics. 2023 Jan 6;15(1):202. [Content Brief]
[2]. Rodríguez-Pascau L, et al. PPAR gamma agonist leriglitazone improves frataxin-loss impairments in cellular and animal models of Friedreich Ataxia. Neurobiol Dis. 2021 Jan;148:105162. [Content Brief]
[3]. Musokhranova U, et al. Mitochondrial modulation with leriglitazone as a potential treatment for Rett syndrome. J Transl Med. 2023 Oct 26;21(1):756. [Content Brief]
[4]. Pizcueta P, et al. Development of PPARγ Agonists for the Treatment of Neuroinflammatory and Neurodegenerative Diseases: Leriglitazone as a Promising Candidate. Int J Mol Sci. 2023 Feb 6;24(4):3201. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.6850 mL | 13.4250 mL | 26.8500 mL | 67.1249 mL |
| 5 mM | 0.5370 mL | 2.6850 mL | 5.3700 mL | 13.4250 mL | |
| 10 mM | 0.2685 mL | 1.3425 mL | 2.6850 mL | 6.7125 mL | |
| 15 mM | 0.1790 mL | 0.8950 mL | 1.7900 mL | 4.4750 mL | |
| 20 mM | 0.1342 mL | 0.6712 mL | 1.3425 mL | 3.3562 mL | |
| 25 mM | 0.1074 mL | 0.5370 mL | 1.0740 mL | 2.6850 mL | |
| 30 mM | 0.0895 mL | 0.4475 mL | 0.8950 mL | 2.2375 mL | |
| 40 mM | 0.0671 mL | 0.3356 mL | 0.6712 mL | 1.6781 mL | |
| 50 mM | 0.0537 mL | 0.2685 mL | 0.5370 mL | 1.3425 mL | |
| 60 mM | 0.0447 mL | 0.2237 mL | 0.4475 mL | 1.1187 mL | |
| 80 mM | 0.0336 mL | 0.1678 mL | 0.3356 mL | 0.8391 mL | |
| 100 mM | 0.0268 mL | 0.1342 mL | 0.2685 mL | 0.6712 mL |
Leriglitazone Related Classifications
HY-117727 Related Classifications
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