1. Cell Cycle/DNA Damage
    NF-κB
    Autophagy
  2. PPAR
    Autophagy

Troglitazone (Synonyms: CS-045)

Cat. No.: HY-50935 Purity: 96.55%
Data Sheet SDS Handling Instructions

Troglitazone is a PPARγ agonist with anti-inflammatory and anti-tumor activity.

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

Troglitazone Chemical Structure

CAS No. : 97322-87-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO $94 In-stock
10 mg $85 In-stock
50 mg $340 In-stock
100 mg $610 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

    Troglitazone purchased from MCE. Usage Cited in: Breast Cancer Res Treat. 2017 Jul 5.

    MDA-MB-231 and Hs578T TNBC ‘‘claudin-1-low’’ cells, and the non-tumorigenic human breast epithelial cell line MCF-10A are treated with 20 μM of TGZ, RGZ, D2-TGZ, or DMSO (Ctrl) for 24 h and subjected to western blot analysis with claudin-1 (CLDN1) antibody. α-tubulin is used as loading control.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Troglitazone is a PPARγ agonist with anti-inflammatory and anti-tumor activity.

    In Vitro

    Troglitazone inhibits the growth of 786-O and A498 cells with EC50 values of 5.71 µM and 8.38 µM[1]. Troglitazone(5 μM) significantly inhibits the CYP2C8-dependent paclitaxel 6a-hydroxylation and CYP2C9-dependent S-warfarin 7-hydroxylation. Troglitazone extensively suppresses CYP2C19-dependent S-mephenytoin 4´-hydroxylation and CYP3A4-dependent testosterone 6b-hydroxylation and moderately influences the CYP1A2- and CYP2B6-dependent 7-ethoxycoumarin O-deethylation, CYP2A6-dependent coumarin 7-hydroxylation and CYP2D6-dependent bufuralol 1´-hydroxylation. CYP2E1-dependent 7-ethoxycoumarin O-deethylation is not inhibited[2].

    In Vivo

    Local hypoxia is observed in liver but not in adipose tissue in troglitazone-treated mice. A significant increase in Ki-67/CD31 LI in liver, BAT, and WAT is observed in the 400 mg/kg troglitazone group[3]. Troglitazone reduces the incidence of diabetes by 16 weeks compared to controls, when administered by gavage from weaning at a dose of 400 mg/kg body weight[4].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT00003058 Dana-Farber Cancer Institute|National Cancer Institute (NCI) Sarcoma June 1997 Phase 2
    NCT00116545 Parke-Davis|National Institute on Aging (NIA) Atherosclerosis|Diabetes Mellitus January 1997 Phase 2|Phase 3
    NCT01055223 GlaxoSmithKline Fractures, Bone|Type II Diabetes May 2009
    View MoreCollapse
    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 2.2648 mL 11.3240 mL 22.6480 mL
    5 mM 0.4530 mL 2.2648 mL 4.5296 mL
    10 mM 0.2265 mL 1.1324 mL 2.2648 mL
    Kinase Assay
    [2]

    Standard incubation mixtures (final volume of 0.20 mL) containe recombinant P450 (0.010 μM) in 50 mM potassium phosphate buåer (pH 7.4) containing an NADPH-generating system (0.5 mm NADP+, 5 mM glucose 6-phosphate, 0.5 unit glucose 6-phosphate dehydrogenase/mL) and substrates (1±100 lM). For determination of CYP1A2, CYP2B6, CYP2E1 and CYP3A4 activities, 100 mM potassium phosphate buffer (pH 7.4) is used. When human liver microsomes are used as the enzyme source, 500, 25, 100 and 25 pmol totalP450 per mL are used for paclitaxel 6a-hydroxylation, S-warfarin 7-hydroxylation,S-mephenytoin 4´-hydroxylation and testosterone 6b-hydroxylation respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    Troglitazone is made at 100 mM concentration in DMSO and added to the culture medium at the final concentration of less than 0.1%.

    The effect of PPARγ ligands on cell proliferation of RCC cells is determined using MTT assay. Briefly, cells of 0.5×l04 cells/well are inoculated into a 96-well plate, treated with pioglitazone or troglitazone at various concentrations. After an incubation for 24 h, 20 µL/well 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT, 5 g/L) is added to each well, the medium is then removed, and 200 µL of 0.04mol/LHCl in isopropanol is added to dissolve the reduced formazan product. The plate is read in a microplate reader at 590 nm. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Troglitazone is prepared daily in vehicle, 0.5% methylcellulose (MC).

    Mice are randomized into two groups of eleven mice each using a weight stratification method, and they are treated with vehicle (0.5 % MC) or 400 mg/kg Troglitazone (TG). Vehicle or TG is administered by oral gavage once daily in the morning, seven days/week for four weeks. The dose volume is 10 mL/kg body weight. Water and food consumption are measured during week 3 of the study, and body weights are measured weekly. After treatment for four weeks, two and a half hours prior to sacrifice, 100 mg/kg HP-1 diluted in saline is injected i.p. into ten mice in each group (10 mL/kg). As the negative control for hypoxia staining, one mouse in each group is injected i.p. with saline. All mice are sacrificed between 9:00 a.m. and 12:00 p.m. by an overdose of nembutal (150 mg/kg of body weight, i.p.). Heart, liver, and interscapular adipose tissue, including BAT and WAT, are removed, and the heart and adipose tissue are weighed prior to fixation. The relative weight of these tissues per body weight is calculated. All tissue is fixed in ice-cold 10% neutral buffered formalin, embedded in paraffin, and sectioned for hematoxylin and eosin staining for histopathological evaluation. A diagnosis of mild mammary ductal hyperplasia is made when there are three cell layers in the mammary gland duct, and a diagnosis of moderate ductal hyperplasia is made when four or more layers are present. Unstained slides are used for immunological detection of tissue hypoxia. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    441.54

    Formula

    C₂₄H₂₇NO₅S

    CAS No.

    97322-87-7

    Storage

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

    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

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

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number

     

    Organization name *

    Country *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Troglitazone
    Cat. No.:
    HY-50935
    Quantity: