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  3. Rosiglitazone

Rosiglitazone  (Synonyms: BRL 49653)

Cat. No.: HY-17386 Purity: 99.90%
COA Handling Instructions

Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone is an TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer.

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

Rosiglitazone Chemical Structure

Rosiglitazone Chemical Structure

CAS No. : 122320-73-4

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 90 publication(s) in Google Scholar

Other Forms of Rosiglitazone:

Top Publications Citing Use of Products

84 Publications Citing Use of MCE Rosiglitazone

WB
IF
Cell Viability Assay

    Rosiglitazone purchased from MedChemExpress. Usage Cited in: Carcinogenesis. 2023 Mar 31;bgad015.  [Abstract]

    Rosiglitazone (ROSI; 15, 30, 60, 120, 240 µM; 24 h) significantly inhibits the growth of NCI-H929 and OPM-2 cells.

    Rosiglitazone purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2019 Jan 15;843:134-144.  [Abstract]

    Protein levels of BACE1 and APP are measured by western blot assay in cerebral cortex of 12-month-old AD mice with different treatments (RSG and GW9662).

    Rosiglitazone purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2019 Jan 15;843:134-144.  [Abstract]

    Protein levels of sAPPα and sAPPβ are measured by western blot assay in cerebral cortex of 12-month-old AD mice with different treatments (RSG and GW9662).

    Rosiglitazone purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2019 Jan 15;843:134-144.  [Abstract]

    PPARγ level is determined by IF assay in 3×Tg-AD mice, 3×Tg-AD mice with RSG treatment, 3×Tg-AD-KO mice, 3×Tg-AD-KO mice with GW9662 stimulation.

    Rosiglitazone purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2018 Aug 21;126:259-268.  [Abstract]

    Laser confocal microscope is performed to measure MMP indicated with the ratio of JC-1 Red/JC-1 Green. Nuclei are counterstained with DAPI (blue). Bar graphs represent the mean ± SD of red/green fluorescence intensity.

    Rosiglitazone purchased from MedChemExpress. Usage Cited in: Front Mol Neurosci. 2017 Sep 14;10:293.  [Abstract]

    Rosiglitazone enhances the phosphorylation of insulin receptor substrate 1 (IRS1, phosphorylated at Ser 636/639), which is considered to be the main activator of the Akt/mTOR pathway by IGF-1R.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone is an TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer[1][2][4][7].

    IC50 & Target[1][2][4]

    PPARγ

    40 nM (Kd)

    PPARγ

    60 nM (EC50)

    TRPC5

    30 μM (EC50)

    TRPM3

     

    In Vitro

    Rosiglitazone (0.1-10 μM, 72 h) results in pluripotent C3H10T1/2 stem cell differentiation to adipocytes[1].
    Rosiglitazone (1 μM, 24 h) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons[3].
    Rosiglitazone (1 μM, 24 h) protects Neuro2A cells and hippocampal neurons against oxidative stress, and up-regulates BCL-2 expression in an NF-α1-dependent manner[3].
    Rosiglitazone (0.01-100 μM, 15 min) inhibits TRPM3 with IC50 values of 9.5 and 4.6 μM against nifedipine- and PregS-evoked activity respectively[4].
    Rosiglitazone (0.5-50 μM, 7 days) inhibits ovarian cancer cell proliferation[7].
    Rosiglitazone (5 μM, 7 days) suppresses Olaparib (HY-10162) induced alterations of cellular senescence and promotes apoptosis in A2780 and SKOV3 cells[7].

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

    Cell Proliferation Assay[7]

    Cell Line: A2780 and SKOV3 cells
    Concentration: 0.5-50 μM
    Incubation Time: 1-7 days
    Result: Inhibited cell proliferation in a time‑dependent and concentration‑dependent manner.

    Western Blot Analysis[3]

    Cell Line: Hippocampal neurons
    Concentration: 1 μM
    Incubation Time: 24 h
    Result: Increased NF-α1 and BCL-2 protein level.
    In Vivo

    Rosiglitazone (oral administration, 5 mg/kg, daily for 8 weeks) decreases the serum glucose in diabetic rats[5].
    Rosiglitazone (intraperitoneal injection, 3 mg/kg/day) ameliorates airway inflammation induced by cigarette smoke via inhibiting the M1 macrophage polarization by activating PPARγ and RXRα in male Wistar rats[6].
    Rosiglitazone (intraperitoneal injection, 10 mg/kg, once every 2 days) inhibits subcutaneous ovarian cancer growth in A2780 and SKOV3 mouse subcutaneous xenograft models[7].

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

    Animal Model: Streptozotocin (STZ)-induced diabetic rats[5]
    Dosage: 5 mg/kg
    Administration: Oral administration, daily for 8 weeks.
    Result: Decreased IL-6, TNF-α, and VCAM-1 levels in diabetic group.
    Displayed lower levels of lipid peroxidation and NOx with an increase in aortic GSH and SOD levels compared to diabetic groups.
    Animal Model: Male Wistar rats[6]
    Dosage: 3 mg/kg/day
    Administration: Intraperitoneal injection, twice a day, 6 days per week for 12 consecutive weeks
    Result: Ameliorated emphysema, elevated PEF, and higher level of total cells, neutrophils and cytokines (TNF-α and IL-1β) induced by cigarette smoke (CS).
    Inhibited CS-induced M1 macrophage polarization and decreased the ratio of M1/M2.
    Clinical Trial
    Molecular Weight

    357.43

    Formula

    C18H19N3O3S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N1)SC(CC2=CC=C(OCCN(C)C3=NC=CC=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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 250 mg/mL (699.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 2 mg/mL (5.60 mM; ultrasonic and warming and heat to 60°C)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7978 mL 13.9888 mL 27.9775 mL
    5 mM 0.5596 mL 2.7978 mL 5.5955 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    Concentration (final)

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    V2

    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    90% Corn Oil

      Solubility: 2.5 mg/mL (6.99 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 2

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (6.99 mM); Clear solution

    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 (27.98 mM); Suspended 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: 99.90%

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 2.7978 mL 13.9888 mL 27.9775 mL 69.9438 mL
    5 mM 0.5596 mL 2.7978 mL 5.5955 mL 13.9888 mL
    DMSO 10 mM 0.2798 mL 1.3989 mL 2.7978 mL 6.9944 mL
    15 mM 0.1865 mL 0.9326 mL 1.8652 mL 4.6629 mL
    20 mM 0.1399 mL 0.6994 mL 1.3989 mL 3.4972 mL
    25 mM 0.1119 mL 0.5596 mL 1.1191 mL 2.7978 mL
    30 mM 0.0933 mL 0.4663 mL 0.9326 mL 2.3315 mL
    40 mM 0.0699 mL 0.3497 mL 0.6994 mL 1.7486 mL
    50 mM 0.0560 mL 0.2798 mL 0.5596 mL 1.3989 mL
    60 mM 0.0466 mL 0.2331 mL 0.4663 mL 1.1657 mL
    80 mM 0.0350 mL 0.1749 mL 0.3497 mL 0.8743 mL
    100 mM 0.0280 mL 0.1399 mL 0.2798 mL 0.6994 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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