Troglitazone (CS-045)

製品コードS8432 バッチS843201

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	88 mg/mL (199.3 mM)
		Ethanol	15 mg/mL (33.97 mM)
		Water	Insoluble
* <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	トログリタゾンは、細胞分化と成長を調節するリガンド活性化転写因子であるペルオキシソーム増殖因子活性化受容体（PPAR）の強力なアゴニストです。トログリタゾンは膀胱がん細胞においてオートファジー、アポトーシス、およびネクロプトーシスを誘導します。トログリタゾンはPfa1細胞におけるRSL3誘発性のフェロトーシスおよび脂質過酸化を防止します。
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. It induces Erk phosphorylation in human prostate cancer cells via a PPARγ-independent signaling pathway. 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.
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. 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. It attenuates pancreatic damage and inflammation in experimental chronic pancreatitis.

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。

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