2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Neuronal Signaling Membrane Transporter/Ion Channel Autophagy Apoptosis
  3. PPAR TRP Channel Autophagy Ferroptosis Apoptosis
  4. 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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10 mM * 1 mL in DMSO
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Customer Review

Based on 82 publication(s) in Google Scholar

Other Forms of Rosiglitazone:

Rosiglitazone Related Antibodies

Top Publications Citing Use of Products

76 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.

    View All PPAR Isoform Specific Products:

    View All Isoforms
    PPARα PPARβ/δ PPARγ PPAR PPARδ

    View All TRP Channel Isoform Specific Products:

    View All Isoforms
    TRPC TRPM TRPV TRPA TRPML

    • 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.

    Rosiglitazone Related Antibodies

    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

    Appearance

    Solid

    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 (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:  0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (27.98 mM); Suspended solution; Need ultrasonic

    • 2.

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

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

    • 3.

      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

    • 4.

      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

    • 5.

      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

    • 6.

      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 MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.90%

    COA (245 KB) HNMR (266 KB) LCMS (268 KB) Elemental Analysis Report (103 KB)

    Handling Instructions (2659 KB)
    References
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    Rosiglitazone Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    Rosiglitazone122320-73-4BRL 49653BRL49653BRL-49653PPARTRP ChannelAutophagyFerroptosisApoptosisPeroxisome proliferator-activated receptorsTransient receptor potential channelsPPARγantihyperglycemicneuroprotectiondiabeticdiabetesmellitusbladdercancerhepatocellularcarcinomaHCCsmokesenescenceovarian cancerInhibitorinhibitorinhibit

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