Pioglitazone HCl

For research use only.

Catalog No.S2046 Synonyms: AD-4833, U-72107E

3 publications

Pioglitazone HCl Chemical Structure

Molecular Weight(MW): 392.9

Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 50 In stock
USD 40 In stock
USD 170 In stock
USD 370 In stock
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Selleck's Pioglitazone HCl has been cited by 3 publications

2 Customer Reviews

  • Primary hepatocytes were treated with or without 20μM Wy14643/Pioglitazone/Rosiglitazone for 24h followed by stimulation with or without 1μg/ml recombinant human FGF21 for 15min. FGF21 signaling was analyzed by phosphorylation of ERK1/2 and FRS2 examination.

    Mol Nutr Food Res, 2017, 61(9). Pioglitazone HCl purchased from Selleck.

    Accumulated 7-day BrdU labeling in representative sections of pancreatic islets from mice fed (A) normal chow, (B) HFD, (C) HFD+clodronate, and (D) HFD+pioglitazone. β-Cells were immunostained with anti-insulin Ab (green) and for replication with anti-BrdU Ab (red). Nuclei were stained in blue. Scale bar, 100 μm. The percentage of BrdU-positive β-cells was calculated. Values are means±SE with 5 pancreas samples in each experimental group analyzed and are shown in E. *P<0.05 where significant difference was detected between the HFD mice and other treatment groups. No significant difference was detected between the results of other groups.

    Endocrinology and Metabolism, 2016, 311(4): E763-E771.. Pioglitazone HCl purchased from Selleck.

Purity & Quality Control

Choose Selective P450 (e.g. CYP17) Inhibitors

Biological Activity

Description Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.
Targets
PPARgamma [1]
In vitro

Pioglitazone inhibits LPS-induced iNOS expression and NO generation, and inhibition of iNOS is sufficient to protect dopaminergic neurons against LPS insult. Pioglitazone protects dopaminergic neurons against LPS insult at least via inhibiting iNOS expression and NO generation, which is potentially mediated via inhibition of p38 MAPK activity. Pioglitazone inhibits LPS-induced phosphorylation of p38 MAPK. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
COS cells NXvOe49TTnWwY4Tpc44h[XO|YYm= MlPUWJJidnOlcnnweIlwdmGuIHHjeIl3[XSrb36gbY4hS0:VIHPlcIx{KGW6cILld5NqdmdiUGDBVkBo[W2vYTDhcoQhWliUIHHsdIhiQyC4YXz1[ZMhcW5idHjlJJBiemWwdHjld4V{KGmwZHnjZZRmeyB7NTWgZ49v\mmmZX7j[UBqdnSnco\hcEwhTUN3ME2wMlQ6KM7:TR?= MWSxNVkxPjJ7Mx?=
HepG2 cells NGryWVhHfW6ldHnvckBie3OjeR?= MVnQ[ZJwgGm|b33lJJBzd2yrZnXyZZRweiCjY4TpeoF1\WRicnXj[ZB1d3JiZ3HtcYEh[WexbnnzeIlkKGGldHn2bZR6KGmwIFjldGczKGOnbHzzMEBGSzVyPUeuOkDPxE1? NILHemEyODdzNEWwNy=>

... Click to View More Cell Line Experimental Data

In vivo Pioglitazone administered orally (0.3-3 mg/kg/d for 7 days) dose dependently reduces hyperglycemia, hyperlipidemia, and hyperinsulinemia in male fatty rats. Pioglitazone improves glucose tolerance and augmentes the glycemic response to exogenous insulin and clearance of plasma triglyceride in rats. [2] Pioglitazone-treated transgenic mice reveals improved muscle strength and body weight, exhibits a delayed disease onset, and survives significantly longer than nontreated SOD1-G93A mice. [3] Pioglitazone markedly decreases hyperglycemia, hyperlipidemia, hyperinsulinemia, and glucoseintolerance characterized as insulin resistant states in these rats and mice. Pioglitazone potentiates insulin-mediated glucose metabolism in the diaphragm and adipose tissues of yellow KK mice and enhanced the glycemic response to exogenous insulin in Zucker fatty rats. [4] Pioglitazone results in a reduction in the number of activated microglia and reactive astrocytes in the hippocampus and cortex of APPV717I transgenic mice. Pioglitazone decreases beta-secretase-1 (BACE1) mRNA and protein levels in APPV717I transgenic mice. [5]

Protocol

Solubility (25°C)

In vitro DMSO 79 mg/mL (201.06 mM)
Water Insoluble
Ethanol ''4 mg/mL

* 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 392.9
Formula

C19H20N2O3S.HCl

CAS No. 112529-15-4
Storage powder
in solvent
Synonyms AD-4833, U-72107E
Smiles CCC1=CN=C(C=C1)CCOC2=CC=C(C=C2)CC3C(=O)NC(=O)S3.Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04501406 Not yet recruiting Drug: Pioglitazone|Other: Placebo Type 2 Diabetes Mellitus (T2DM)|Nonalcoholic Steatohepatitis University of Florida|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) August 15 2020 Phase 2
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 Unknown status Drug: Pioglitazone|Other: Placebo Chronic Kidney Diseases The University of Texas at Arlington April 1 2018 Phase 4
NCT03080480 Terminated 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

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P450 (e.g. CYP17) Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID