Pioglitazone

Alias: AD-4833; Pioglitazone Hydrochloride; Pioglitazone HCl; Actos; U-72107A; AD-4833; pioglitazone; pioglitazone hydrochloride; U 72107A; U-72107A; U72,107A
Cat No.:V0828 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.
Pioglitazone Chemical Structure CAS No.: 111025-46-8
Product category: PPAR
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
Other Sizes

Other Forms of Pioglitazone:

  • Pioglitazone D4
  • Pioglitazone HCl
  • Pioglitazone potassium
  • Pioglitazone-d4 (alkyl)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product 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.

Biological Activity I Assay Protocols (From Reference)
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].
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].
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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H20N2O3S
Molecular Weight
356.44
CAS #
111025-46-8
Related CAS #
Pioglitazone-d4;1134163-29-3;Pioglitazone hydrochloride;112529-15-4;Pioglitazone potassium;1266523-09-4;Pioglitazone-d4 (alkyl);1134163-31-7
SMILES
O=C(N1)SC(CC2=CC=C(OCCC3=NC=C(CC)C=C3)C=C2)C1=O
Synonyms
AD-4833; Pioglitazone Hydrochloride; Pioglitazone HCl; Actos; U-72107A; AD-4833; pioglitazone; pioglitazone hydrochloride; U 72107A; U-72107A; U72,107A
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)
Solubility Data
Solubility (In Vitro)
DMSO: 15 mg/mL (42.1 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
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.

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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.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.


 (Please use freshly prepared in vivo formulations for optimal results.)
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.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Clinical Trial Information
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
Biological Data
  • 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.
  • 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.
  • 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.
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