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  3. Pioglitazone

Pioglitazone  (Synonyms: U 72107)

Cat. No.: HY-13956 Purity: 99.81%
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Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research.

For research use only. We do not sell to patients.

Pioglitazone Chemical Structure

Pioglitazone Chemical Structure

CAS No. : 111025-46-8

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 79 In-stock
Solution
10 mM * 1 mL in DMSO USD 79 In-stock
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5 mg USD 46 In-stock
10 mg USD 72 In-stock
50 mg USD 132 In-stock
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Customer Review

Based on 27 publication(s) in Google Scholar

Other Forms of Pioglitazone:

Top Publications Citing Use of Products

    Pioglitazone purchased from MedChemExpress. Usage Cited in: Inflammation. 2020 Apr;43(2):568-578.  [Abstract]

    Colonic lysates of CON + Veh, DSS + Veh, and DSS + PIO (day 7, day 14, and day 21) group mice are analyzed by immunoblotting with p-ERK, ERK, p-P65, and P65 antibodies, respectively. Each lane represents one mouse.

    Pioglitazone purchased from MedChemExpress. Usage Cited in: Inflammation. 2020 Apr;43(2):568-578.  [Abstract]

    Colonic lysates of CON + Veh, DSS + Veh, and DSS + PIO (day 7, day 14, and day 21) group mice are analyzed by immunoblotting with IL-6, TNF-α, MMP9, and PPARγ antibodies, respectively. Each lane represents one mouse.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research[2][3][4].

    IC50 & Target[1]

    hPPARγ

    0.93 μM (EC50)

    mouse PPARγ

    0.99 μM (EC50)

    hPPARδ

    43 μM (EC50)

    hPPARα

    100 μM (EC50)

    mouse PPARα

    100 μM (EC50)

    In Vitro

    Pioglitazone (0.5 or 1 μM, 5 days) can completely prevent AGEs (advanced glycation end-products)-induced β-cell necrosis and the increase of caspase-3 thereby avoiding the impaired viability caused by AGEs in pancreatic beta cell line HIT-T15[2].
    ? Pioglitazone (1 μM, 1 h) can stimulate insulin secretion induced by low glucose concentration and attenuate the GSSG/GSH ratio in cells cultured with AGEs[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Pioglitazone (oral gavage, 10 or 30 mg/kg, once daily, 14 days) can induce improvements in insulin resistance and diabetes that may be lipocalin-dependent in the liver but not in skeletal muscle[3].
    ? Pioglitazone (oral gavage, 10 mg/kg, once daily, 4 weeks) can significantly reduce body weight (BW), cardiac hypertrophy, elevated blood glucose levels and improve the associated dyslipidemia[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: ob/ob and adipo-/- ob/ob mice with a C57Bl/6 background[3]
    Dosage: 10 or 30 mg/kg
    Administration: Oral gavage; once daily; 14 days
    Result: Showed 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 significantly reduced to a similar degree at 30 mg/kg.
    Also showed no changes of expressions of TNFα and resistin in adipose tissues of ob/ob and adipo-/- ob/ob mice at 10 mg/kg but decreased at 30 mg/kg.
    Animal Model: Male Wistar albino rats[4]
    Dosage: 10 mg/kg
    Administration: Oral gavage; once daily; 4 weeks
    Result: Decreased 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.
    Clinical Trial
    Molecular Weight

    356.44

    Formula

    C19H20N2O3S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N1)SC(CC2=CC=C(OCCC3=NC=C(CC)C=C3)C=C2)C1=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (70.14 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.08 mg/mL (5.84 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (28.06 mM); Suspened solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.81%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.8055 mL 14.0276 mL 28.0552 mL 70.1380 mL
    5 mM 0.5611 mL 2.8055 mL 5.6110 mL 14.0276 mL
    10 mM 0.2806 mL 1.4028 mL 2.8055 mL 7.0138 mL
    15 mM 0.1870 mL 0.9352 mL 1.8703 mL 4.6759 mL
    20 mM 0.1403 mL 0.7014 mL 1.4028 mL 3.5069 mL
    25 mM 0.1122 mL 0.5611 mL 1.1222 mL 2.8055 mL
    30 mM 0.0935 mL 0.4676 mL 0.9352 mL 2.3379 mL
    40 mM 0.0701 mL 0.3507 mL 0.7014 mL 1.7535 mL
    50 mM 0.0561 mL 0.2806 mL 0.5611 mL 1.4028 mL
    60 mM 0.0468 mL 0.2338 mL 0.4676 mL 1.1690 mL
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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