MedChemExpress - Model Leriglitazone -146062-44-4
Leriglitazone (MIN-102; Hydroxypioglitazone) is an orally active and a BBB-penatrable 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[1][2][3][4].MCE products for research use only. We do not sell to patients.
Leriglitazone
MCE China：Leriglitazone
Brand：MedChemExpress (MCE)
Cat. No.HY-117727
CAS：146062-44-4
Synonyms：MIN-102; Hydroxypioglitazone
Purity：99.23%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping：Room temperature in continental US; may vary elsewhere.
Description：Leriglitazone (MIN-102; Hydroxypioglitazone) is an orally active and a BBB-penatrable 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.
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].
In Vivo：Leriglitazone (50 mg/kg; Feed administration; 8 months) improves motor impairment in a Friedreich ataxia mouse model[2]. Leriglitazone (75 mg/kg; Feed administration; 7 months) has an improved effect in Rett mouse model[3].
IC50 & Target：PPAR-γ 9 μM (EC50)
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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]
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