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

Rosiglitazone hydrochloride (Synonyms: BRL 49653 hydrochloride)

Cat. No.: HY-17386A
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Rosiglitazone hydrochloride (BRL 49653 hydrochloride) is a selective, orally active PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively. Rosiglitazone hydrochloride binds to PPARγ with a Kd of approximately 40 nM. Rosiglitazone hydrochloride is also an activator of TRPC5 (EC50=~30 μM) and an inhibitor of TRPM3.

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

Rosiglitazone hydrochloride Chemical Structure

Rosiglitazone hydrochloride Chemical Structure

CAS No. : 302543-62-0

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Top Publications Citing Use of Products

    Rosiglitazone hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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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    Description

    Rosiglitazone hydrochloride (BRL 49653 hydrochloride) is a selective, orally active PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively. Rosiglitazone hydrochloride binds to PPARγ with a Kd of approximately 40 nM. Rosiglitazone hydrochloride is also an activator of TRPC5 (EC50=~30 μM) and an inhibitor of TRPM3[1][2][3][4].

    IC50 & Target[1]

    PPARγ1

    30 nM (EC50)

    PPARγ2

    100 nM (EC50)

    TRPC5

     

    TRPM2

     

    TRPM3

     

    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].

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

    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].

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

    Molecular Weight

    393.89

    Formula

    C₁₈H₂₀ClN₃O₃S

    CAS No.

    302543-62-0

    SMILES

    [H]Cl.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

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
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    Keywords:

    RosiglitazoneBRL 49653BRL49653BRL-49653PPARTRP ChannelAutophagyFerroptosisPeroxisome proliferator-activated receptorsTransient receptor potential channelsPPARγantihyperglycemicneuroprotectiondiabeticdiabetesmellitusbladdercancerhepatocellularcarcinomaHCCInhibitorinhibitorinhibit

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