For research use only.
Catalog No.S2046 Synonyms: AD-4833, U-72107E
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.
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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.
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Choose Selective P450 (e.g. CYP17) Inhibitors
|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.|
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. 
|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.  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.  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.  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. |
-  Xing B, et al. J Neuroinflammation,?008, 5, 4.
-  Sugiyama Y, et al. Arzneimittelforschung,?990, 40(3), 263-267.
-  Sch黷z B, et al. J Neurosci,?005, 25(34), 7805-7812.
|In vitro||DMSO||79 mg/mL (201.06 mM)|
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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