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

Rosiglitazone (Synonyms: BRL49653)

Cat. No.: HY-17386 Purity: 99.46%
Handling Instructions

Rosiglitazone is a peroxisome proliferator-activated receptor-gamma (PPAR-γ) agonist, and is a blocker of TRPM2 and TRPM3 channels.

For research use only. We do not sell to patients.
Rosiglitazone Chemical Structure

Rosiglitazone Chemical Structure

CAS No. : 122320-73-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
50 mg USD 60 In-stock
200 mg USD 180 In-stock
500 mg   Get quote  
1 g   Get quote  

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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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References


    Rosiglitazone is a peroxisome proliferator-activated receptor-gamma (PPAR-γ) agonist, and is a blocker of TRPM2 and TRPM3 channels.

    IC50 & Target

    TRPM2 and TRPM3 blocker[1]
    PPAR agonist[2]

    In Vitro

    TRPM2 is unaffected by Rosiglitazone at concentrations up to 10 μM but is inhibited completely at higher concentrations (IC50~22.5 μM). TRPC5 is strongly stimulated by Rosiglitazone at concentrations of 10 μM and greater (EC50~30 μM). Low concentrations of Rosiglitazone (0.1-1 μM) cause about 20 % inhibition of TRPM3. Higher concentrations of Rosiglitazone cause stronger and complete TRPM3 inhibition with IC50 values of 9.5 μM and 4.6 μM against nifedipine- and PregS-evoked activity[1]. Rosiglitazone is a peroxisome proliferator-activated receptor-γ (PPARγ) agonist, which is an anti-diabetic agent against type 2 diabetes[2].

    In Vivo

    Rosiglitazone prevents Endotoxin lethality by attenuating HMGB1 release. BALB/c mice (n=10-11 per group) are injected with a single dose of Rosiglitazone (10 mg/kg, i.p.) with or without GW9662 (1 mg/kg, i.p.), followed 30 min later by a lethal infusion of Endotoxin (LPS, 10 mg/kg, i.p.)[3].

    Clinical Trial
    Preparing Stock Solutions
    Concentration Volume 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.
    Cell Assay

    Rosiglitazone is dissolved in DMSO and stored, and then diluted with appropriate medium before use[2].

    Human neuroblastoma SH-SY5Y cells are maintained in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum, 100 μg/mL Streptomycin and 100 U/mL Penicillin G. SH-SY5Y cells are transfected with the longest isoform of human tau (2N4R) tagged with GFP using lipofectamine. 24 hr after transfection, cells are treated with Rosiglitazone (10 μM, 50 μM) for 24 hr[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration

    Rosiglitazone is prepared in DMSO, and then diluted in 0.5% carboxymethyl cellulose in drinking water to maximize solubility.

    OLETF rats are divided randomly into two groups (n=6 or 7 animals per group) at 21 weeks of age. Rats are given standard rat food or rat food supplemented with 3 mg/kg/day Rosiglitazone for 27 weeks. Urinary glucose is monitored weekly using Diastix. Individual rats are diagnosed as diabetic when positive glycosuria is identified. C57BL6 mice are divided randomly into two groups (n=7 animals per group) at 10 weeks of age. Mice received a single intraperitoneal injection of 150 mg/kg of STZ in 0.5 M sodium citrate buffer and, after 3 days, 3 mg/kg of Rosiglitazone or vehicle are daily administered per os for 4 consecutive days. Mice with glycemia over 11 mM glucose are diagnosed as diabetic.
    BALB/c mice are randomly assigned to one of four groups: injection of LPS (10 mg/kg), injection of LPS (10 mg/kg) plus Rosiglitazone (10 mg/kg), injection of LPS (10 mg/kg) plus Rosiglitazone (10 mg/kg) plus GW9662 (1 mg/kg), or injection of GW9662 (1 mg/kg) alone. Another group of BALB/c mice are treated with Rosiglitazone (10 mg/mL) after LPS (10 mg/kg) infusion. Mortality is recorded for up to 2 weeks after LPS injection to ensure that no additional late deaths occurred. For measurement of plasma HMGB1 levels, BALB/c mice are subjected to sepsis by LPS injection in the presence or absence of Rosiglitazone. After 20 h, blood is collected, allowed to clot for 2 h at room temperature, and then centrifuged for 20 min at 1,500 g. The levels of circulating HMGB1 in serum are determined by Western blot analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight




    CAS No.


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

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 180 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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