Pioglitazone HCl

Catalog No.S2046 Batch:S204603

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Technical Data

Formula

C19H20N2O3S.HCl
Molecular Weight 392.9 CAS No. 112529-15-4
Solubility (25°C)* In vitro DMSO 78 mg/mL (198.52 mM)
Ethanol 4 mg/mL (10.18 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.)

Preparing Stock Solutions

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
Ferroptosis [8] hPPARγ [1]
(Cell-free assay)		 rPPARγ [6]
(Cell-free assay)		 CYP2C8 [7]
(Cell-free assay)		 CYP3A4 [7]
(Cell-free assay)		 View More
0.93 μM(EC50) 0.99 μM(EC50) 1.7 μM(Ki) 11.8 μM(Ki)
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]
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 (from reference)

Customer Product Validation

, , Mol Nutr Food Res, 2017, 61(9)

Data from [Data independently produced by , , Endocrinology and Metabolism, 2016, 311(4): E763-E771.]

Selleck's Pioglitazone HCl has been cited by 10 publications

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
The downregulation of miR-129-5p relieves the inflammatory response in acute respiratory distress syndrome by regulating PPARγ-mediated autophagy [ Ann Transl Med, 2022, 10(6):345] PubMed: 35433953
Rubicon promotes the M2 polarization of Kupffer cells via LC3-associated phagocytosis-mediated clearance to improve liver transplantation [ Cell Immunol, 2022, 378:104556] PubMed: 35700602
Exosomes derived from pioglitazone-pretreated MSCs accelerate diabetic wound healing through enhancing angiogenesis [ J Nanobiotechnology, 2021, 19(1):150] PubMed: 34020670
The Function of PPARγ/AMPK/SIRT-1 Pathway in Inflammatory Response of Human Articular Chondrocytes Stimulated by Advanced Glycation End Products. [ Biol Pharm Bull, 2019, 42(8):1303-1309] PubMed: 31366866
Activation of PPARγ pathway enhances cellular anti-oxidant capacity to protect long-term cultured primary rat neural cells from apoptosis [ Nan Fang Yi Ke Da Xue Xue Bao, 2019, 39(1):23-29] PubMed: 30692062
N-3 polyunsaturated fatty acids increase hepatic fibroblast growth factor 21 sensitivity via a PPAR-γ-β-klotho pathway. [Yang W, et al. Mol Nutr Food Res, 2017, 10.1002/mnfr.201601075] PubMed: 28371258
The Role of Bile Salt Export Pump (BSEP) Gene Repression in Drug-Induced Cholestatic Liver Toxicity [Brandy Garzel, et al. Drug Metab Dispos, 2013, 42(3):318-22] PubMed: 24335466

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.