A PPARγ agonist (EC50 = ~500-600 nM for both human and murine PPARγ); selective for PPARγ over PPARα exhibiting low level activation of PPARα at 1 µM and 5.4-fold activation at a concentration of 10 µM; reduces hyperglycemia

Pioglitazone – 50 mg

Brand:
Cayman
CAS:
111025-46-8
Storage:
-20
UN-No:
Non-Hazardous - /

Pioglitazone is an agonist of the peroxisome proliferator-activated receptor γ (PPARγ; EC50 = ~500-600 nM for both human and murine PPARγ).{10857,10670} It is selective for PPARγ over PPARα, exhibiting low level activation of PPARα at 1 µM and 5.4-fold activation at a concentration of 10 µM.{10857} Pioglitazone inhibits pyruvate oxidation and glucose production in hepatocytes when used at a concentration of 10 μM.{37440} In vivo, pioglitazone (0.3-3 mg/kg per day) reduces hyperglycemia, hyperlipidemia, and hyperinsulinemia in a dose-dependent manner in male Wistar fatty rats.{37441} It reduces the number of lesions in a transgenic rat adenocarcinoma of prostate (TRAP) model.{37442} Pioglitazone (2.5 mg/kg) also decreases production of neuroinflammatory cytokines and reduces immobility in the forced swim and tail suspension tests in a mouse model of chronic mild stress, indicating antidepressant-like activity that can be reversed by the PPARγ antagonist GW9662 (Item No. 70785).{37443}  

 

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Description

A PPARγ agonist (EC50 = ~500-600 nM for both human and murine PPARγ); selective for PPARγ over PPARα exhibiting low level activation of PPARα at 1 µM and 5.4-fold activation at a concentration of 10 µM; reduces hyperglycemia, hyperlipidemia, and hyperinsulinemia in a dose-dependent manner in male Wistar fatty rats from 0.3-3 mg/kg; reduces the number of lesions in a TRAP model; decreases production of neuroinflammatory cytokines and reduces immobility in the forced swim and tail suspension tests in a mouse model of chronic mild stress at 2.5 mg/kg

Formal name: 5-[[4-[2-(5-ethyl-2-pyridinyl)ethoxy]phenyl]methyl]-2,4-thiazolidinedione

Synonyms:  U-72107

Molecular weight: 356.4

CAS: 111025-46-8

Purity: ≥98%

Formulation: A crystalline solid

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