Catalog No.S2590

Pioglitazone  Chemical Structure

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.

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In DMSO USD 130 In stock
USD 97 In stock
USD 170 In stock
USD 370 In stock
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Cited by 8 Publications

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  • 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.

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Biological Activity

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.
PPARγ [2]
In vitro

Pioglitazone is metabolised mainly by CYP2C8 and to a lesser extent by CYP3A4 in vitro. [1]

Methods Test Index PMID
Western blot

PubMed: 29972411     

Representative western bolotting trace of VEGFR-2 and phospho-VEGFR-2 (Tyr1175) protein levels in rat neonatal cardiomyocytes under hypertrophic stimuli, and treated with 0, 10, 20 (µM) pioglitazone for 24 hours.

Phopsho-RB / RB; 

PubMed: 25264247     

Pioglitazone treatment causes a decrease in the levels of phosphorylated RB in both NCI-H2347 and NCI-H1993 cells within 24 hours.

29972411 25264247
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. [2] 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. [3] 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. [4] 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. [5]


Solubility (25°C)

In vitro DMSO 10 mg/mL (28.05 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 356.44


CAS No. 111025-46-8
Storage powder
in solvent
Synonyms N/A

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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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PPAR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID