Molecular Weight(MW): 356.44
Pioglitazone is a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist, used to treat diabetes; A weak activator for full-length hPPARα, but not full-length hPPARδ.
Cited by 8 Publications
5 Customer Reviews
PPARγ activation, but not PPARα activation, increases β-klotho expression and FGF21 signaling. Protein (A) levels of β-klotho in hepatocytes after stimulation with or without 20μM Wy14643/Pioglitazone/Rosiglitazone for 24h
Mol Nutr Food Res, 2017, doi: 10.1002/mnfr.201601075. Pioglitazone purchased from Selleck.
Repression of BSEP gene expression upon treatment with reported BSEP inhibitors in human primary hepatocytes. BSEP mRNA expression was measured using real-time PCR in hepatocytes from at least three donors upon treatment with BSEP inhibitors as described in Materials and Methods (A). Dotted lines indicate 20% (dark) and 60% (light) BSEP repression compared with vehicle control (0.1% DMSO). A standard MTT assay as described in Materials and Methods was performed in human primary hepatocytes to monitor cytotoxicities associated with BSEP inhibitors at selected concentrations (B). All the data are expressed as mean±S.D. (n = 3).
Drug Metab Dispos, 2014, 42(3):318-22.. Pioglitazone purchased from Selleck.
RAW264.7 cells and hPBMCs were stimulated with RGZ (10 μmol/liter), pioglitazone (PGZ, 10 μmol/liter), or both. The integrin αV and β5 mRNA (I) or protein (J) levels were examined by RT-qPCR or immunoblotting.
J Biol Chem, 2019, 293(43):16572-16582. Pioglitazone purchased from Selleck.
Macrophage (MΦ) staining in representative sections of pancreatic islets from mice fed (A) normal chow, (B) high-fat diet (HFD), (C) HFD + clodronate, and (D) HFD + pioglitazone. β-Cells were immunostained with anti-insulin Ab (green) and MΦs with anti-F4/80 Ab (red). Nuclei were stained in blue. Scale bar, 50 μm. Most of the F4/80-positive cells are detected within the islets.
Am J Physiol Endocrinol Metab, 2016, 311(4):E763-E771. . Pioglitazone purchased from Selleck.
Caco2 cells were treated with different concentrations (10 or 20 lg/ml) of a PPARc agonist (pioglitazone) (d) for 6 h without UA stimulation. SIRT1, PGC-1, PPARc and ABCG2 were measured, and quantitative analyses of the results are shown. The data are presented as the mean ± SEM. *p<0.05 and **p<0.01 compared with the control group.
Endocrine, 2016, 53(2):443-52. . Pioglitazone purchased from Selleck.
Purity & Quality Control
Choose Selective PPAR Inhibitors
|Description||Pioglitazone is a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist, used to treat diabetes; A weak activator for full-length hPPARα, but not full-length hPPARδ.|
Pioglitazone is metabolised mainly by CYP2C8 and to a lesser extent by CYP3A4 in vitro. 
|In vivo||Pioglitazone significantly attenuates left ventricular (LV) cavity dilatation and dysfunction by echocardiography as well as LV end-diastolic pressure in mice with extensive anterior myocardial infarction. Pioglitazone partially normalizes LV dP/dt(max) and dP/dt(min), indices of LV contractile function, which are significantly reduced in MI mice.  Pioglitazone results in a reduced activation of microglia, reduced induction of iNOS-positive cells and less glial fibrillary acidic protein positive cells in both striatum and substantia nigra pars compacta of MPTP mouse model of Parkinson's disease. Pioglitazone almost completely blocks staining of TH-positive neurons for nitrotyrosine, a marker of NO-mediated cell damage.  Pioglitazone (approximately 20 mg/kg/day) attenuates the MPTP-induced glial activation and prevents the dopaminergic cell loss in the substantia nigra pars compacta (SNpc) in MPTP mouse model of Parkinson's disease.  Pioglitazone results in a reduction in the number of activated microglia and reactive astrocytes in the hippocampus and cortex of 10-month-old APPV717I transgenic mice. Pioglitazone treatment reduces the expression of the proinflammatory enzymes cyclooxygenase 2 (COX2) and inducible nitric oxide synthase (iNOS). Pioglitazone decreases beta-secretase-1 (BACE1) mRNA and protein levels, and also a 27% reduction in the levels of soluble Abeta1-42 peptide. |
-  Jaakkola T, et al. Basic Clin Pharmacol Toxicol,?006, 99(1), 44-51.
-  Shiomi T, et al. Circulation,?002, 106(24), 3126-3132.
-  Dehmer T, et al. J Neurochem,?004, 88(2), 494-501.
|In vitro||DMSO||10 mg/mL (28.05 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00904046||Recruiting||Drug: Pioglitazone|Drug: Placebo||Uric Acid Kidney Stone Disease||University of Texas Southwestern Medical Center|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|Takeda Pharmaceuticals North America Inc.||September 5 2019||Not Applicable|
|NCT03501277||Completed||Drug: Alogliptin|Drug: Pioglitazone|Drug: SYR-322-4833 BL||Healthy Volunteers||Takeda||May 26 2018||Phase 1|
|NCT03471117||Recruiting||Drug: Pioglitazone|Other: Placebo||Chronic Kidney Diseases||The University of Texas at Arlington||April 1 2018||Phase 4|
|NCT03080480||Recruiting||Drug: Pioglitazone||Chronic Granulomatous Disease||Children''s Hospital of Fudan University||September 1 2017||Phase 1|Phase 2|
|NCT02585765||Withdrawn||Drug: Pioglitazone|Drug: Placebo||Spinal Cord Injury|Pressure Ulcers||James J. Peters Veterans Affairs Medical Center||February 1 2017||Phase 2|
|NCT02889003||Recruiting||Drug: Pioglitazone + TKI||Chronic Myeloid Leukemia (CML)||Versailles Hospital|Pr Philippe ROUSSELOT||December 2016||Phase 2|
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