Troglitazone is a PPARγ agonist, with EC₅₀s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively.

Troglitazone is a PPARγ agonist, with EC₅₀s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively^[1]. Troglitazone (2-200 μM) 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. Troglitazone (50 μM) increases chromatin condensation in MIA Paca2 and PANC-1 cells, enhances the activity of caspase-3 and decreases Bcl-2 expression^[2]. Troglitazone (0, 1, 2, and 4 μM) sensitizes TRAIL-mediated apoptosis in human lung adenocarcinoma cells. Troglitazone enhancement of TRAIL-induced apoptosis is blocked by inhibition of autophagy, via activation of autophagy flux. In addition, the effects of troglitazone are induced by PPARγ activation in A549 cells^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Troglitazone (200 mg/kg, p.o.) shows inhibitory effects on the growth of tumor in the MIA Paca2 xenograft model^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

441.54

C₂₄H₂₇NO₅S

97322-87-7

曲格列酮；特洛格列酮

Room temperature in continental US; may vary elsewhere.

DMSO : 160 mg/mL (362.37 mM; Need ultrasonic)

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——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
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• 1.

  请依序添加每种溶剂： 0.5% CMC-Na  0.5% Tween-80

  Solubility: 10 mg/mL (22.65 mM); Suspended solution; Need ultrasonic
• 2.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.66 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 3.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.66 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 4.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (5.66 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.66 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [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.