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    InvivoChem Cat #: V0828
    CAS #: 111025-46-8Purity ≥98%

    Description: Pioglitazone (U-72107A; AD-4833; Actos; AD4833, U-72107E) is approved and thiazolidinedione-based anti-diabetic drug which acts as a selective PPARϒ (Peroxisome proliferator-activated receptor γ) agonist with hypoglycemic activity. It inhibits PPARϒ with EC50s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. 

    References: Basic Clin Pharmacol Toxicol. 2006 Jul;99(1):44-51; Circulation. 2002 Dec 10;106(24):3126-32.

    Related CAS #111025-46-8 (free); 112529-15-4 (HCl);  

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    Molecular Weight (MW)356.44
    CAS No.111025-46-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 15 mg/mL (42.1 mM)
    Water:<1 mg/mL
    Ethanol: <1 mg/mL
    SynonymsAD-4833; Pioglitazone Hydrochloride; Pioglitazone HCl; Actos; U-72107A; AD-4833; pioglitazone; pioglitazone hydrochloride; U 72107A; U-72107A; U72,107A

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    In Vitro

    In vitro activity: 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.

    Cell Assay: In order to evaluate cell proliferation, HIT-T15 cells are seeded on 96-well plates (3×104 cells/well) and cultured for 5 days as described. Viable cells are determined using the Cell Titer 96 Aqueous One Solution Cell Proliferation Assay. To evaluate cell apoptosis and cell necrosis, HIT-T15 cells are plated on 6-well dishes (7×105 cells/well) for 5 days in standard conditions (CTR) or in the presence of AGEs (AGEs) with or without Pioglitazone (0.5 or 1 μM) or AG (1 mM). They are then processed to measure both the activity of caspase-3 and the activity of lactate dehydrogenase (LDH) (a stable cytosolic enzyme that is a marker of cell membrane damage and cell death due to necrosis) using Cytotox 96 Non Radioactive Cytotoxicity Assay.

    In VivoPioglitazone 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.
    Animal modelMice and rats
    Formulation & DosageMice: 10 mg/kg Pioglitazone HCl or vehicle (0.25% carboxymethylcellulose) is adnimistered to ob/ob and adipo-/- ob/ob mice by oral gavage once daily for 14 consecutive days. 30 mg/kg Pioglitazone or vehicle is also adnimistered to ob/ob and adipo-/- ob/ob mice by oral gavage once daily for 14 consecutive days. 
    Rats: Male Wistar albino rats (weighing 250±20 g) are ued.Rats that achieved serum glucose level ≥250 mg/dL and serum creatinine level ≥1.5 mg/dL are divided into 2 groups (n=10 per each group): diabetic nephropathic (DN) group in which rats received an equal amount of vehicle (0.5% carboxy methyl cellulose) and Pioglitazone-treated (DN+Pio) group in which rats treated with Pioglitazone. Pioglitazone (10 mg/kg BW) is given orally by gastric gavage, once daily, for 4 weeks.

    J Neuroinflammation. 2008 Jan 18;5:4. doi: 10.1186/1742-2094-5-4; Arzneimittelforschung. 1990 Mar;40(3):263-7; J Neurosci. 2005 Aug 24;25(34):7805-12.

    These protocols are for reference only. InvivoChem does not independently validate these methods.


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