1. Cell Cycle/DNA Damage
    Neuronal Signaling
    Membrane Transporter/Ion Channel
    Autophagy
    Apoptosis
  2. PPAR
    TRP Channel
    Autophagy
    Ferroptosis
    Apoptosis
  3. Rosiglitazone

Rosiglitazone (Synonyms: BRL 49653)

Cat. No.: HY-17386 Purity: 99.90%
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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10 mM * 1 mL in DMSO USD 66 In-stock
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Customer Review

Based on 52 publication(s) in Google Scholar

Other Forms of Rosiglitazone:

Top Publications Citing Use of Products

47 Publications Citing Use of MCE Rosiglitazone

    Rosiglitazone purchased from MCE. Usage Cited in: Front Mol Neurosci. 2017 Sep 14;10:293.

    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.

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

    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 MCE. Usage Cited in: Eur J Pharmacol. 2019 Jan 15;843:134-144.

    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 MCE. Usage Cited in: Eur J Pharmacol. 2019 Jan 15;843:134-144.

    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 MCE. Usage Cited in: Eur J Pharmacol. 2019 Jan 15;843:134-144.

    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.

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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].

    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].

    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.
    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)

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

    H2O : < 0.1 mg/mL (ultrasonic) (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
    10 mM 0.2798 mL 1.3989 mL 2.7978 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    • 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

    • 3.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

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

    • 4.

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

      Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution

    • 5.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.90%

    References
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    Product Name:
    Rosiglitazone
    Cat. No.:
    HY-17386
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