Troglitazone is an orally active PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively. Troglitazone has anticancer activity, prevents and inhibits the development of type 2 diabetes.
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Troglitazone Chemische Struktur
CAS. Nr. : 97322-87-7
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Based on 21 publication(s) in Google Scholar
Other Forms of Troglitazone:
Troglitazone-d4
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Troglitazone purchased from MedChemExpress. Usage Cited in:
Yonsei Med J. 2018 Nov;59(9):1096-1106.
[Abstract]
MCN and N2a cells are treated with Control (DMSO), Troglitazone (Tro; 20 µM), or GW9662 (10 µM) for 24 h, followed by detection of PPAR-γ protein level via Western blot assay.
Troglitazone purchased from MedChemExpress. Usage Cited in:
Breast Cancer Res Treat. 2017 Oct;165(3):517-527.
[Abstract]
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.
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Beschreibung
Troglitazone is an orally active PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively. Troglitazone has anticancer activity, prevents and inhibits the development of type 2 diabetes.
IC50 & Target[1]
PPARγ
550 nM (EC50, Human PPARγ)
In Vitro
Troglitazone (2-200 μM, 24 h) is cytotoxic to the pancreatic cancer cell lines (MIA Paca2 and PANC-1 cells), with IC50s of 49.9±1.2 and 51.3±5.3 μM, respectively[2].
Troglitazone (50 μM, 24 h) increases chromatin condensation in MIA Paca2 and PANC-1 cells, enhances the activity of caspase-3 and decreases Bcl-2 expression[2].
Troglitazone (0-4 μM, 12 h) sensitizes TRAIL-mediated apoptosis in human lung adenocarcinoma cells (A549, HCC-15 and
Calu-3)[3].
Troglitazone (0-4 μM, 12 h) induces autophagy and sensitized apoptosis mediated by TRAIL in A549 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Troglitazone Related Antibodies
In Vivo
Troglitazone (200 mg/kg, p.o., every day for 5 weeks) shows inhibitory effects on the growth of tumor in the MIA Paca2 xenograft model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Room temperature in continental US; may vary elsewhere.
Speicherung
Powder
-20°C
3 years
In solvent
-80°C
1 year
-20°C
6 months
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 125 mg/mL (283.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
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
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 900 μLCorn oil, and mix evenly.
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution.
If precipitation or phase separation occurs during preparation,
heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 0.5% CMC-Na/0.5% Tween-80 in Saline water
Solubility: 10 mg/mL (22.65 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[1]. Willson TM, et al. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50.
[Content Brief]
[2]. Fujita M, et al. In vitro and in vivo cytotoxicity of troglitazone in pancreatic cancer. J Exp Clin Cancer Res. 2017 Jul 3;36(1):91.
[Content Brief]
[3]. Nazim UM, et al. PPARγ activation by troglitazone enhances human lung cancer cells to TRAIL-induced apoptosis via autophagy flux. Oncotarget. 2017 Apr 18;8(16):26819-26831.
[Content Brief]
[4]. Knowler WC, et al. Prevention of type 2 diabetes with troglitazone in the Diabetes Prevention Program. Diabetes. 2005 Apr;54(4):1150-6.
[Content Brief]
Zellassay
[2]
Briefly, cells are seeded into 96-well plates at a density of 1 × 105 cells/well and incubated for 24 h. The cells are treated with Troglitazone in the presence or absence of other chemicals for a further 24 h using FBS-free medium. The assay utilizes the conversion of alamar blue reagent to fluorescent resorufin by metabolically active cells. The resorufin signal is measured at an excitation wavelength of 530 nm and an emission wavelength of 580 nm. The 50% growth inhibitory concentrations (IC50) are calculated according to the sigmoid inhibitory effect model E = IC50 γ/(IC50 γ + Cγ), where E represents the surviving fraction (% of control), C represents the drug concentration in the medium, and γ represents the Hill coefficient. For co-exposure studies, the Troglitazone dosage is set to approximately the IC50 value for each cell line[2].
MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
Tierverwaltung
[2]
Balb/c male mice (4 weeks old) are subcutaneously inoculated in the back with MIA Paca2 cells (5 × 106 cells/100 μL in PBS) 14 days prior to starting Troglitazone administration. Mice are then orally administered 200 mg/kg Troglitazone in 0.5% methylcellulose solution or vehicle daily for 5 weeks. Tumor size is measured bi-dimensionally and the volume is calculated using the formula (length × width2) × 0.5. Body weights of mice are also monitored throughout the experiment[2].
MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
Verweise
[1]. Willson TM, et al. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50.
[Content Brief]
[2]. Fujita M, et al. In vitro and in vivo cytotoxicity of troglitazone in pancreatic cancer. J Exp Clin Cancer Res. 2017 Jul 3;36(1):91.
[Content Brief]
[3]. Nazim UM, et al. PPARγ activation by troglitazone enhances human lung cancer cells to TRAIL-induced apoptosis via autophagy flux. Oncotarget. 2017 Apr 18;8(16):26819-26831.
[Content Brief]
[4]. Knowler WC, et al. Prevention of type 2 diabetes with troglitazone in the Diabetes Prevention Program. Diabetes. 2005 Apr;54(4):1150-6.
[Content Brief]
[1]. Willson TM, et al. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50.
[2]. Fujita M, et al. In vitro and in vivo cytotoxicity of troglitazone in pancreatic cancer. J Exp Clin Cancer Res. 2017 Jul 3;36(1):91.
[3]. Nazim UM, et al. PPARγ activation by troglitazone enhances human lung cancer cells to TRAIL-induced apoptosis via autophagy flux. Oncotarget. 2017 Apr 18;8(16):26819-26831.
[4]. Knowler WC, et al. Prevention of type 2 diabetes with troglitazone in the Diabetes Prevention Program. Diabetes. 2005 Apr;54(4):1150-6.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO
1 mM
2.2648 mL
11.3240 mL
22.6480 mL
56.6200 mL
5 mM
0.4530 mL
2.2648 mL
4.5296 mL
11.3240 mL
10 mM
0.2265 mL
1.1324 mL
2.2648 mL
5.6620 mL
15 mM
0.1510 mL
0.7549 mL
1.5099 mL
3.7747 mL
20 mM
0.1132 mL
0.5662 mL
1.1324 mL
2.8310 mL
25 mM
0.0906 mL
0.4530 mL
0.9059 mL
2.2648 mL
30 mM
0.0755 mL
0.3775 mL
0.7549 mL
1.8873 mL
40 mM
0.0566 mL
0.2831 mL
0.5662 mL
1.4155 mL
50 mM
0.0453 mL
0.2265 mL
0.4530 mL
1.1324 mL
60 mM
0.0377 mL
0.1887 mL
0.3775 mL
0.9437 mL
80 mM
0.0283 mL
0.1416 mL
0.2831 mL
0.7078 mL
100 mM
0.0226 mL
0.1132 mL
0.2265 mL
0.5662 mL
Troglitazone 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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