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Pioglitazone potassium (U-72107) is a PPARγ (peroxisome proliferator-activated receptor) agonist with anti-diabetic effects. It has EC50s of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively.
ln Vitro |
The pancreatic β-cell line T15 can avoid AGEs-induced HIT-impaired cell viability by totally preventing AGEs-induced β-cell necrosis and the rise of caspase-3, with pioglitazone potassium (0.5 or 1 μM, 5 days) being the most effective treatment to prevent these events [2]. Pioglitazone potassium (1 μM, 1 h) can lower the GSSG/GSH ratio in AGE-cultured cells and increase insulin secretion triggered by low glucose concentrations [2].
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ln Vivo |
Pioglitazone potassium (oral gavage, 10 or 30 mg/kg once daily for 14 days) reduces insulin resistance and diabetes, perhaps in a lipocalin-dependent way in the liver but not in skeletal muscle[3] . Pioglitazone potassium (oral gavage, 10 mg/kg, once day, 4 weeks) can dramatically reduce body weight (BW), cardiac hypertrophy, increased blood glucose levels and ameliorate associated dyslipidemia [4].
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Animal Protocol |
Animal/Disease Models: ob/ob and adipo-/- ob/ob mice on C57Bl/6 background [3]
Doses: 10 or 30 mg/kg Route of Administration: po (oral gavage); one time/day; 14-day Experimental Results: ob/ Serum free fatty acid and triglyceride levels and adipocyte size were unchanged in ob and adipo-/- ob/ob C57BL/6 mice at the 10 mg/kg dose, but were Dramatically diminished to similar levels at the 10 mg/kg dose. degree. 30 mg/kg. It was also shown that the expression of TNFα and resistin in the adipose tissue of ob/ob and adipo-/- ob/ob mice was unchanged at the 10 mg/kg dose but diminished at the 30 mg/kg dose. Animal/Disease Models: Male Wistar albino rat [4] Doses: 10 mg/kg Route of Administration: po (oral gavage); one time/day; 4-week Experimental Results: Reduce elevated serum creatinine and creatine kinase MB (CK-MB) levels, TGF-β1 gene expression and regulates the expression of MMP-2/TIMP-2 system. |
References |
[1]. Kenji Kuwabara, 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 l
[2]. A Puddu, 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]. Naoto Kubota, 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]. Rania A Elrashidy, 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. |
Molecular Formula |
C19H21KN2O3S
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Molecular Weight |
396.544944524765
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CAS # |
1266523-09-4
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Related CAS # |
Pioglitazone;111025-46-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C(C1C=CC(OCCC2N=CC(CC)=CC=2)=CC=1)C1SC(=O)NC1=O.[KH]
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5218 mL | 12.6088 mL | 25.2175 mL | |
5 mM | 0.5044 mL | 2.5218 mL | 5.0435 mL | |
10 mM | 0.2522 mL | 1.2609 mL | 2.5218 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.