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 (hydrochloride) – 5 g

Brand:
Cayman
CAS:
112529-15-4
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 GW 9662 (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, monohydrochloride

Synonyms: 

Molecular weight: 392.9

CAS: 112529-15-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Endocrinology & Metabolism|Hormones & Receptors|PPARs||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Dyslipidemias||Research Area|Immunology & Inflammation

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