Pioglitazone

Catalog No.S2590 Batch:S259003

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Technical Data

Formula

C19H20N2O3S

Molecular Weight 356.44 CAS No. 111025-46-8
Solubility (25°C)* In vitro DMSO 23 mg/mL (64.52 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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.
Targets
PPARγ [2]
In vitro

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

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]

Protocol (from reference)

Animal Study:

[3]

  • Animal Models

    Male C57/Bl6 mice

  • Dosages

    20 mg/kg

  • Administration

    p.o.

Customer Product Validation

, , Mol Nutr Food Res, 2017, doi: 10.1002/mnfr.201601075

, , Drug Metab Dispos, 2014, 42(3):318-22.

Data from [Data independently produced by , , J Biol Chem, 2019, 293(43):16572-16582]

Data from [Data independently produced by , , Am J Physiol Endocrinol Metab, 2016, 311(4):E763-E771. ]

Selleck's Pioglitazone has been cited by 34 publications

Characterization of ferroptosis-triggered pyroptotic signaling in heart failure [ Signal Transduct Target Ther, 2024, 9(1):257] PubMed: 39327446
PPAR-γ agonists reactivate the ALDOC-NR2F1 axis to enhance sensitivity to temozolomide and suppress glioblastoma progression [ Cell Commun Signal, 2024, 22(1):266] PubMed: 38741139
Upregulation of PGC-1α expression by pioglitazone mediates prevention of sepsis-induced acute lung injury [ Braz J Med Biol Res, 2024, 57:e13235] PubMed: 38511769
Mitigation of non-alcoholic steatohepatitis via recombinant Orosomucoid 2, an acute phase protein modulating the Erk1/2-PPARγ-Cd36 pathway [ Cell Rep, 2023, 42(7):112697] PubMed: 37355990
Molecular Signature Predictive of Long-Term Liver Fibrosis Progression to Inform Antifibrotic Drug Development [ Gastroenterology, 2022, 162(4):1210-1225] PubMed: 34951993
Artificial intelligence-rationalized balanced PPARα/γ dual agonism resets dysregulated macrophage processes in inflammatory bowel disease [ Commun Biol, 2022, 5(1):231] PubMed: 35288651
Adipose Rheb deficiency promotes miR-182-5p expression via the cAMP/PPARγ signaling pathway [ J Genet Genomics, 2022, S1673-8527(22)00133-3] PubMed: 35550871
FGF21 attenuates pulmonary arterial hypertension via downregulation of miR-130, which targets PPARγ [ J Cell Mol Med, 2022, 10.1111/jcmm.17154] PubMed: 34989130
Peroxisome proliferator-activated receptor-γ ameliorates neuronal ferroptosis after traumatic brain injury in mice by inhibiting cyclooxygenase-2 [ Exp Neurol, 2022, 354:114100] PubMed: 35490721
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] PubMed: 35207746

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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