Leriglitazone hydrochloride
Based on 1 Customer Validation
Leriglitazone (MIN-102; Hydroxypioglitazone) hydrochloride is an orally active and a BBB-penetrable PPARγ agonist with an EC50 of 9 μM. Leriglitazone hydrochloride, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone hydrochloride can be used in the study of neuroinflammatory and neurodegenerative diseases.
For research use only. We do not sell to patients.
- Purity: 99.64%
- CAS No.: 146062-46-6
- Formula: C19H21ClN2O4S
- Molecular Weight:408.90
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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PPAR-γ 9 μM (EC50) |
Leriglitazone (100 nM; 45 days) hydrochloride increases PKAN astrocyte activity and respiratory activity, and reduces iron accumulation[1].
Leriglitazone (50-500 nM; 5 days) hydrochloride 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) hydrochloride prevents lipid droplet accumulation in frataxin-deficient cardiomyocytes[2].
Leriglitazone (100-500 nM; 48 h) hydrochloride 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.
Leriglitazone (75 mg/kg; Feed administration; 7 months) hydrochloride 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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 146062-46-6
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Appearance Solid
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Molecular Weight 408.90
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Formula C19H21ClN2O4S
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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.[H]Cl
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Synonyms
MIN-102 hydrochloride; Hydroxypioglitazone hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 50 mg/mL (122.28 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Purity & Documentation
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Data Sheet (273 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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Handling Instructions (2659 KB)
References
[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 (sealed storage, away from moisture). 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 | 2.4456 mL | 12.2279 mL | 24.4559 mL | 61.1396 mL |
| 5 mM | 0.4891 mL | 2.4456 mL | 4.8912 mL | 12.2279 mL | |
| 10 mM | 0.2446 mL | 1.2228 mL | 2.4456 mL | 6.1140 mL | |
| 15 mM | 0.1630 mL | 0.8152 mL | 1.6304 mL | 4.0760 mL | |
| 20 mM | 0.1223 mL | 0.6114 mL | 1.2228 mL | 3.0570 mL | |
| 25 mM | 0.0978 mL | 0.4891 mL | 0.9782 mL | 2.4456 mL | |
| 30 mM | 0.0815 mL | 0.4076 mL | 0.8152 mL | 2.0380 mL | |
| 40 mM | 0.0611 mL | 0.3057 mL | 0.6114 mL | 1.5285 mL | |
| 50 mM | 0.0489 mL | 0.2446 mL | 0.4891 mL | 1.2228 mL | |
| 60 mM | 0.0408 mL | 0.2038 mL | 0.4076 mL | 1.0190 mL | |
| 80 mM | 0.0306 mL | 0.1528 mL | 0.3057 mL | 0.7642 mL | |
| 100 mM | 0.0245 mL | 0.1223 mL | 0.2446 mL | 0.6114 mL |
Leriglitazone hydrochloride Related Classifications
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