1. Cell Cycle/DNA Damage
    Membrane Transporter/Ion Channel
    Autophagy
  2. PPAR
    TRP Channel
    Autophagy

Rosiglitazone (Synonyms: BRL49653)

Cat. No.: HY-17386 Purity: 99.21%
Handling Instructions

Rosiglitazone (BRL49653) is a potent thiazolidinedione insulin sensitizer. Rosiglitazone is a selective PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively.

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
Estimated Time of Arrival: December 31
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Estimated Time of Arrival: December 31
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Customer Review

Other Forms of 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. 2018 Nov 6. pii: S0014-2999(18)30653-8. 

    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. 2018 Nov 6. pii: S0014-2999(18)30653-8. 

    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. 2018 Nov 6. pii: S0014-2999(18)30653-8. 

    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

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Rosiglitazone (BRL49653) is a potent thiazolidinedione insulin sensitizer. Rosiglitazone is a selective PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively.

    IC50 & Target[1]

    PPARγ1

    30 nM (EC50)

    PPARγ2

    100 nM (EC50)

    In Vitro

    Rosiglitazone is a potent and selective activator of PPARγ, with EC50s of 30 nM and 100 nM for PPARγ1 and PPARγ2, respectively, and a Kd of appr 40 nM for PPARγ. Rosiglitazone (BRL49653, 0.1, 1,10 μM) promotes differentiation of C3H10T1/2 stem cells to adipocytes[1]. Rosiglitazone (Compound 6) activates PPARγ, with an EC50 of 60 nM[2]. Rosiglitazone (1 μM) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons. Rosiglitazone (1 μM) also protects Neuro2A cells and hippocampal neurons against oxidative stress, and up-regulates BCL-2 expression in an NF-α1-dependent manner[3]. Rosiglitazone completely inhibits TRPM3 with IC50 values of 9.5 and 4.6 μM against nifedipine- and PregS-evoked activity, but such effects are not via PPARγ. Rosiglitazone inhibits TRPM2 at higher concentration, with an IC50 of appr 22.5 μM. Rosiglitazone is a strong stimulator of TRPC5 channels, with an EC50 of ∼30 μM[4].

    In Vivo

    Rosiglitazone (5 mg/kg, p.o.) decreases the serum glucose in diabetic rats. Rosiglitazone also decreases IL-6, TNF-α, and VCAM-1 levels in diabetic group. Rosiglitazone in combination with losartan increases glucose compared to diabetic and Los-treated groups. Rosiglitazone significantly ameliorates endothelial dysfunction indicated by a significantly lower contractile response to PE and Ang II and enhancement of ACh-provoked relaxation in aortas isolated from diabetic rats[5].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 180 mg/mL (503.60 mM)

    *"≥" means soluble, but saturation unknown.

    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.
    References
    Kinase Assay
    [1]

    cDNA encoding amino acids 174-475 of PPARγ1 is amplified via polymerase chain reaction and inserted into bacterial expression vector pGEX-2T. GST-PPARγ LBD is expressed in BL21(DE3)plysS cells and extracts. For saturation binding analysis, bacterial extracts (100 μg of protein) are incubated at 4°C for 3 h in buffer containing 10 mM Tris (pH 8.0), 50 mM KCl, 10 mM dithiothreitol with [3H]-BRL49653 (specific activity, 40 Ci/mmol) in the presence or absence of unlabeled Rosiglitazone. Bound is separated from free radioactivity by elution through 1-mL Sephadex G-25 desalting columns. Bound radioactivity eluted in the column void volume and is quantitated by liquid scintillation counting[1].

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

    Cell Assay
    [1]

    C3H10T1/2 cells are grown in a 24-well plate in DME medium supplemented with 10% fetal calf serum. Medium and compound (Rosiglitazone) are exchanged every 3 days. Cells are stained at day 7 with Oil Red O and photographed[1].

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

    Animal Administration
    [2]

    Rats are intravenously injected with 38 mg/kg streptozotocin and after 48 h, diabetes is identified by urinary glucosuria and then random blood sugar is measured and this day is regarded as day 0. Animals with a serum glucose level of 220-300 mg/dL are selected to be used in this study. Rats are randomly separated into five groups for daily drug administration for 8 weeks: group 1: control nondiabetic rats given a vehicle only (0.5 mL/kg of 0.5% carboxy methyl celleluse orally), group 2: control diabetic rats given a vehicle, group 3: diabetic rats receiving Rosiglitazone (5 mg/kg orally), group 4: diabetic rats receiving losartan (2 mg/kg, orally), and group 5: diabetic rats receiving both Rosiglitazone and losartan[2].

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

    References
    Molecular Weight

    357.43

    Formula

    C₁₈H₁₉N₃O₃S

    CAS No.

    122320-73-4

    SMILES

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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

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

    Cat. No.: HY-17386