Troglitazone

製品コードS8432 バッチS843202

印刷

化学情報

Synonyms

CS-045, Romglizone

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₄H₂₇NO₅S

分子量

441.54

CAS No.

97322-87-7

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

88 mg/mL (199.3 mM)

Ethanol (warmed with 50ºC water bath)

6 mg/mL (13.58 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.400mg/ml (9.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 88 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.700mg/ml (1.59mM)	Taking the 1 mL working solution as an example, add 50 μL of 14 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells. Troglitazone prevents RSL3-induced ferroptosis and lipid peroxidation in Pfa1 cells.
in vitro	Troglitazone significantly inhibits cell growth by cell cycle arrest and apoptotic cell death. This compound also downregulates surface expression of CD97, a novel dedifferentiation marker, in FTC-133 cells and upregulated sodium iodide symporter (NIS) mRNA in TPC-1 and FTC-133 cells. This PPARγ agonist induces antiproliferation and redifferentiation in thyroid cancer cell lines^[1]. It induces Erk phosphorylation in human prostate cancer cells via a PPARγ-independent signaling pathway^[2]. TGZ up-regulates nitric oxide synthesis, induces the p53 pathway, inhibits cholesterol biosynthesis, induces p21 cyclin-dependent kinase inhibitor, has antioxidant function, and activates extracellular signal-regulated protein kinase (ERK) in a PPARγ-independent manner. This chemical induces Egr-1 expression by transcriptional and post-transcriptional regulation. Egr-1 induction by this compound results in the increase of binding affinity and transactivation of the promoter containing Egr-1 consensus sequences, thereby possibly inducing other anti-tumorigenic proteins^[3].
in vivo	Troglitazone is an effective antidiabetic drug with a fundamentally new mechanism of action. However, within a year after its widespread use, individual cases of liver injury and failure are reported^[5]. This compound significantly inhibits tumor growth of human colorectal cancer cells (HCT-116), human breast cancer cells (MCF-7), and human prostate cancer cells (PC-3) in immunodeficient mice^[3]. It attenuates pancreatic damage and inflammation in experimental chronic pancreatitis^[4].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Thyroid cancer cell lines TPC-1, FTC-133, FTC-236, FTC-238, XTC-1 and ARO82-1 cell lines
	濃度	5, 10, 20, 40 μM
	反応時間	0, 2, 4, and 6 days
	実験の流れ	Growth experiments are done in a 96-well plate in hexaplicate. Cells at 85%-100% confluency are harvested with 1×Trypsin/EDTA solution and seeded into a 96-well plate at 3-5×10³ cells per well depending upon growth rate and maintained in 200 μL H5 medium in a humidified incubator. After 24 hours, cells are incubated with different concentrations of troglitazone and the media was changed daily. Colorometric dimethyl-thiazol-diphenyltetrazolium bromide (MTT) proliferation assays are performed at 0, 2, 4, and 6 days after treatment. MTT (400 μg/mL) is added to each well and incubated for 3 hours. It is solubilized with 0.04 N HCl/iso-propanol/3% SDS and incubated for 1 hour. The optical densities in the 96-well plates are determined using an enzyme-linked immunosorbent assay (ELISA) microplate reader at 595 nm/620 nm.
動物実験	動物モデル	C57BL/6 mice
	投薬量	0.2% (with chow)
	投与方法	oral administration

参考

https://pubmed.ncbi.nlm.nih.gov/15785241/
https://pubmed.ncbi.nlm.nih.gov/22448169/
https://pubmed.ncbi.nlm.nih.gov/12475986/

https://pubmed.ncbi.nlm.nih.gov/15743784/
https://pubmed.ncbi.nlm.nih.gov/17575588/
https://pubmed.ncbi.nlm.nih.gov/27842070/

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Unveiling the shield: Troglitazone's impact on epilepsy-induced nerve injury through ferroptosis inhibition [ CNS Neurosci Ther, 2024, 30(8):e14911]	PubMed: 39145422
Adipocyte‑rich microenvironment promotes chemoresistance via upregulation of peroxisome proliferator‑activated receptor gamma/ABCG2 in epithelial ovarian cancer [ Int J Mol Med, 2024, 53(4)37]	PubMed: 38426604
pH-dependent rearrangement determines the iron-activation and antitumor activity of artemisinins [ Free Radic Biol Med, 2021, 163:234-242]	PubMed: 33359684
Capsaicin up-regulates pro-apoptotic activity of thiazolidinediones in glioblastoma cell line [ Biomed Pharmacother, 2020, 132:110741]	PubMed: 33038582
RORγ Is a Targetable Master Regulator of Cholesterol Biosynthesis in a Cancer Subtype [ Nat Commun, 2019, 11;10(1):4621]	PubMed: 31604910

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。