Pioglitazone HCl

A PPARγ agonist

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10mg

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货号: ajci6546
CAS: 112529-15-4
别名: 盐酸吡格列酮,U 72107A; AD 4833
分子式: C19H20N2O3S.HCl
分子量: 392.9
纯度: >98%
溶解度: ≥ 19.65 mg/mL in DMSO, ≥ 7.52 mg/mL in EtOH with ultrasonic and warming
储存: Store at -20°C
库存: 现货

Background

Pioglitazone HCl is a potent and highly selective agonist of PPARγ with IC50 value of 3μM[1].

Pioglitazone HCl can increase both insulin-stimulated glucose uptake in peripheral tissues and insulin sensitivity in hepatic and adipose tissue. It is treated for hyperglycemia and Type 2 diabetes (T2D). Pioglitazone needs insulin as a co-factor for PPAR agonism so it is not effect when being treated to late stages of T2D with developed insulinopenia. In clinical trials, 15mg pioglitazone produces significant improvements in HbA1c and fasting plasma glucose (FPG) [2].

Pioglitazone is also reported to have multiple beneficial effects on lipid metabolism. It produces significant decreases in TG and significant increases in high density lipoprotein (HDL) in clinical studies [2].

参考文献:
[1] Saad S, Agapiou DJ, Chen XM, Stevens V, Pollock CA. The role of Sgk-1 in the upregulation of transport proteins by PPAR-{gamma} agonists in human proximal tubule cells. Nephrol Dial Transplant. 2009 Apr;24(4):1130-41.
[2] Dorkhan M, Frid A. A review of pioglitazone HCL and glimepiride in the treatment of type 2 diabetes. Vasc Health Risk Manag. 2007;3(5):721-31.

Protocol

Cell experiment:

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[2].

Animal experiment:

Mice[3] 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[4] 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.

参考文献:

[1]. Kuwabara K, et al. A novel selective peroxisome proliferator-activated receptor alpha agonist, 2-methyl-c-5-[4-[5-methyl-2-(4-methylphenyl)-4-oxazolyl]butyl]-1,3-dioxane-r-2-carboxylic acid (NS-220), potently decreases plasma triglyceride and glucose leve
[2]. Puddu A, et al. Pioglitazone attenuates the detrimental effects of advanced glycation end-products in the pancreatic beta cell line HIT-T15. Regul Pept. 2012 Aug 20;177(1-3):79-84.
[3]. Kubota N, et al. Pioglitazone ameliorates insulin resistance and diabetes by both adiponectin-dependent and -independent pathways. J Biol Chem. 2006 Mar 31;281(13):8748-55.
[4]. Elrashidy RA, et al. Pioglitazone attenuates cardiac fibrosis and hypertrophy in a rat model of diabetic nephropathy. J Cardiovasc Pharmacol Ther. 2012 Sep;17(3):324-33.