Size | Price | Stock | Qty |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
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.
ln Vitro |
Advanced glycation end products (AGEs) can cause β-cell necrosis and an increase in caspase-3. Pioglitazone (0.5 or 1 μM, 5 days) can entirely prevent these effects, preventing AGEs from impairing the viability of the pancreatic β-cell line HIT-T15. Pioglitazone (1 μM, 1 h) can lower the GSSG/GSH ratio in AGE-cultured cells and increase insulin secretion that is triggered by low glucose concentrations [2].
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ln Vivo |
Pioglitazone, taken orally once daily for 14 days at a dose of 10 or 30 mg/kg, improves diabetes and insulin resistance; this effect may be lipocalin-dependent in the liver but not in the skeletal muscle [3]. Pioglitazone (oral gavage, 10 mg/kg, once daily, for four weeks) can alleviate dyslipidemia associated with it, raise blood glucose levels, and considerably reduce body weight (BW) and cardiac hypertrophy [4].
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Animal Protocol |
Animal/Disease Models: ob/ob and adipo-/- ob/ob mice with a C57Bl/6 background[3]
Doses: 10 or 30 mg/kg Route of Administration: po (oral gavage); one time/day; 14 days Experimental Results: demonstrated no changes of serum- free fatty acid and triglyceride levels as well as adipocyte sizes in ob/ob and adipo-/- ob/ob C57BL/6 mice at 10 mg/kg but Dramatically decreased to a similar degree at 30 mg/kg. Also demonstrated no changes of expressions of TNFα and resistin in adipose tissues of ob/ob and adipo-/- ob/ob mice at 10 mg/kg but diminished at 30 mg/kg. Animal/Disease Models: Male Wistar albino rats[4] Doses: 10 mg/kg Route of Administration: po (oral gavage); one time/day; 4 weeks Experimental Results: diminished the elevated serum levels of both creatinine and creatine kinase-MB (CK-MB), TGF-β1 gene expression and regulated the expression of MMP-2/TIMP-2 system. |
References |
[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. |
Molecular Formula |
C19H20N2O3S
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Molecular Weight |
356.44
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CAS # |
111025-46-8
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Related CAS # |
Pioglitazone-d4;1134163-29-3;Pioglitazone hydrochloride;112529-15-4;Pioglitazone potassium;1266523-09-4;Pioglitazone-d4 (alkyl);1134163-31-7
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(N1)SC(CC2=CC=C(OCCC3=NC=C(CC)C=C3)C=C2)C1=O
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Synonyms |
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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 |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (5.84 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 10 mg/mL (28.06 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), Suspened solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8055 mL | 14.0276 mL | 28.0552 mL | |
5 mM | 0.5611 mL | 2.8055 mL | 5.6110 mL | |
10 mM | 0.2806 mL | 1.4028 mL | 2.8055 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04501406 | Recruiting | Drug: Pioglitazone Other: Placebo |
Type 2 Diabetes Mellitus (T2DM) Nonalcoholic Steatohepatitis |
University of Florida | December 15, 2020 | Phase 2 |
NCT05775380 | Recruiting | Drug: Pioglitazone 45 mg | Myocardial Reperfusion Injury | University of Campinas, Brazil | June 15, 2023 | Phase 4 |
NCT03080480 | Terminated | Drug: Pioglitazone | Chronic Granulomatous Disease | Children's Hospital of Fudan University | September 1, 2017 | Phase 1 Phase 2 |
NCT04535700 | Completed | Drug: Pioglitazone 30 mg Other: standard of care |
Type 2 Diabetes | Fundacion para la Investigacion Biomedica del Hospital Universitario Ramon y Cajal |
September 18, 2020 | Phase 4 |
Cardiac level of malondialdehyde (MDA) in the different studied groups. N indicates normal rats; D, diabetic rats; DN, diabetic nephropathic rats received vehicle; DN + Pio, diabetic nephropathic rats treated with pioglitazone (10 mg/kg/d). Data are means ± standard deviation (n = 8 per group). *P < .05 versus N, #P < .05 versus D, aP < .05 versus DN. td> |
Cardiac expression of TGF-β1 mRNA (A), MMP-2 mRNA (B), and TIMP-2 mRNA (C) in the different studied groups. TGF-β1 indicates transforming growth factor-β1; MMP-2, matrix metalloproteinase 2; TIMP-2, tissue inhibitor of metalloproteinase 2; M, DNA ladder; N, normal rats; D, diabetic rats; DN, diabetic nephropathic rats received vehicle; DN + Pio, diabetic nephropathic rats treated with pioglitazone (10 mg/kg/d). Data are means ± standard deviation (n = 6 per group). *P < .05 versus N; #P < .05 versus D; aP < .05 versus DN. td> |
Histopathological examination and morphometrical analysis of LV sections of the experimental rats. A, Representative photomicrographs of LV sections stained by Masson’s trichrome stain (×400). Blue staining demonstrates collagen fibers. B, Quantification of interstitical fibrosis. The area percentage of interstitical fibrosis was determined based on the area of fibrosis divided by the total area. C, Myocyte cross-sectional areas in LV tissues of the experimental rats. N, normal rats; D, diabetic rats; DN diabetic nephropathic rats received vehicle; DN + Pio, diabetic nephropathic rats treated with piolitazone (10 mg/kg/d); LV left ventricles. Data are means ± standard deviation (n = 3-4 per group). *P < .05 versus N; #P < .05 versus D; aP < .05 versus DN. td> |