Troglitazone

別名: CS-045, Romglizone 中文名稱：曲格列酮

目錄號：S8432 Purity: 99.47%

Troglitazone是PPAR的有效激動劑，PPAR是配體激活的轉(zhuǎn)錄因，可參與調(diào)解細胞分化和生長。Troglitazone 誘導膀胱癌細胞自噬、凋亡和壞死。Troglitazone 可在Pfa1細胞中防止RSL3誘導的鐵死亡和脂質(zhì)過氧化。

Troglitazone Chemical Structure

CAS: 97322-87-7

規(guī)格	價格	庫存
10mM (1mL in DMSO)	1040.13	現(xiàn)貨
10mg	958.57	現(xiàn)貨
50mg	3661.39	現(xiàn)貨
200mg	9582.31	現(xiàn)貨
1g	32679	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.47%

99.47

Troglitazone相關產(chǎn)品

相關靶點	PPARα PPARβ/δ PPARγ PPARδ	點擊展開
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細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息
ST-13 cells	Function assay	5 μM	11 days	Induction of preadipocyte differentiation in mouse ST-13 cells assessed as lipid accumulation at 5 uM within 11 days by oil red-staining relative to control	19268587
HepG2 cells	Function assay	50 μM	24 h	Induction of p53 protein level in human HepG2 cells at 50 uM up to 24 hrs by immunoblot analysis	25851939
HEK293 cells	Function assay	10 μM	24 h	Transactivation of PPAR-gamma transfected in HEK293 cells at 10 uM after 24 hrs by luciferase reporter gene assay	22579484
HepG2 cells	Function assay	0.5-12.5 μM		Agonist activity at PPARgamma in human HepG2 cells assessed as down-regulation of glucose-6-phosphatase at 0.5 to 12.5 uM by real-time PCR method	22342624
HepG2 cells	Function assay	0.5-12.5 μM		Agonist activity at PPARgamma in human HepG2 cells assessed as down-regulation of phosphoenolpyruvate carboxykinase at 0.5 to 12.5 uM by real-time PCR method	22342624
MA104 cells	Cytotoxicity assay		24 h	Cytotoxicity against monkey MA104 cells after 24 hrs, TD50=18.5 μM	22365411
MDA-MB-231 cells	Proliferation assay		24 h	Antiproliferative activity hormone-independent human MDA-MB-231 cells after 24 hrs by luminescent cell viability assay, IC50=15.7 μM	22409968
MCF7 cells	Proliferation assay		24 h	Antiproliferative activity hormone-dependent human MCF7 cells after 24 hrs by luminescent cell viability assay, IC50=35.4 μM	22409968
HepG2 cells	Function assay		20 h	Transactivation of GAL4-fused PPARgamma LBD expressed in HepG2 cells after 20 hrs by luminescence assay, EC50=0.73 μM	22381047
LNCAP cells	Cytotoxicity assay		24 h	Cytotoxicity against human LNCAP cells after 24 hrs by MTT assay, IC50=22 μM	22546208
PC3 cells	Cytotoxicity assay		24 h	Cytotoxicity against human PC3 cells after 24 hrs by MTT assay, IC50=30 μM	22546208
CHO cells	Function assay		24 h	Agonist activity at human PPARgamma expressed in CHO cells co-transfected with pGL3-PPRE3-TK-luc assessed as transactivation after 24 hrs by firefly luciferase reporter gene assay, EC50=0.44 μM	22342624
HepG2 (DPX-2) cells	Function assay		24 h	Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis, EC50=6.9 μM	20966043
3T3-L1 cells	Function assay			Effective concentration for 50% enhancement of insulin-induced triglyceride accumulation in 3T3-L1 cells, EC50=0.13 μM	9599241
PC12 cells	Proliferation assay			Concentration required for 50% inhibition of cell proliferation in PC12 cells using sulforhodamine B assay, IC50=15 Μm	15109648
A549	Growth inhibition assay			Inhibition of human lung cancer cell line (A549) by 50% in sulforhodamine B assay, GI50=15 μM	15454234
3T3L1 cells	Function assay			Increase in 2-deoxyglucose uptake in mouse 3T3L1 cells at 3 uM by liquid scintillation counter	18477507
HEK293 cells	Function assay			Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with steroid receptor coactivator-1 by EYFP based reporter gene assay	16680159
CV-1 cells	Function assay			Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells, EC50=0.53703 μM	9836620
3T3L1 cells	Function assay			Agonist activity at PPARgamma in mouse 3T3L1 cells, EC50=1 μM	21493073
HepG2 cells	Function assay			Agonist activity at PPARgamma in human HepG2 cells assessed as downregulation of phosphoenolpyruvate carboxykinase mRNA by RT-PCR analysis	22424300
HEK293T cells	Function assay			Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis, IC50=4.5 Μm	23122865
HepG2 cells	Function assay			Agonist activity at PPARgamma in human HepG2 cells assessed as downregulation of glucose-6-phosphatase mRNA by RT-PCR analysis	22424300
HEK293 cells	Function assay			Activation of PPARgamma transfected in HEK293 cells after 18 hrs by firefly luciferase reporter gene-based luminescence assay relative to control, EC50=0.4 μM	21800856
rat ventricular myocytes	Function assay			Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes, IC50=9.5 μM	22761000
CV1 cells	Function assay			Transactivation of human PPARgamma expressed in african green monkey CV1 cells by luciferase reporter gene assay, EC50=0.4 μM	22579420
CHO cells	Function assay			Agonist activity at human recombinant PPARgamma expressed in CHO cells cotransfected with pGL3-PPRE3-TK-luc reporter assessed as beta-galactosidase activity at after 24 hrs by luciferase based transactivation assay, EC50=0.44 μM	22424300
HepG2 cells	Function assay			Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells after 20 hrs by luciferase reporter gene assay, EC50=0.72 μM	23031596
點擊查看更多細胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點

Ferroptosis ^[6]

PPAR ^[1]

體外研究(In Vitro)
體外研究活性	Troglitazone通過阻滯細胞周期和引起細胞凋亡性死亡，顯著地抑制細胞生長。在FTC-133細胞中，下調(diào)CD97（新型去分化標記）的表面表達；在TPC-1和FTC-133細胞中，上調(diào)鈉碘轉(zhuǎn)運體NIS mRNA。Troglitazone作為PPARγ激動劑，誘導甲狀腺癌細胞的抗增殖和重分化作用^[1]。在人類前列腺癌細胞中，Troglitazone不依賴于PPARγ信號通路，誘導Erk磷酸化^[2]。TGZ(Troglitazone)上調(diào)NOS，誘導p53通路，抑制膽固醇合成，誘導依賴于p21 cyclin的激酶抑制劑，具有抗氧化功能，以不依賴于PPARγ的機制激活ERK。TGZ還能通過轉(zhuǎn)錄和轉(zhuǎn)錄后調(diào)節(jié)，誘導Egr-1的表達，并增強含Egr-1共有序列的啟動子的結(jié)合親和力及反式激活活性，因而誘導其他抗腫瘤發(fā)生蛋白的生成^[3]。
細胞實驗	細胞系	甲狀腺癌細胞TPC-1, FTC-133, FTC-236, FTC-238, XTC-1和ARO82-1細胞
	濃度	5, 10, 20, 40 μM
	孵育時間	0, 2, 4, 6天
	方法	收集融合率達到85%-100%的細胞，將其以3-5×10³個細胞/孔的密度接種于96孔板中，培養(yǎng)于200μL/孔的H5培養(yǎng)基中。37℃培養(yǎng)24小時后，用不同濃度的troglitazone對細胞進行處理，每天更換新的培養(yǎng)基。在處理后0,2,4,6天時，進行MTT增殖檢測。將MTT（400 μg/mL）加入每孔，并孵育3小時。然后將其溶解于0.04 N HCl/iso-propanol/3% SDS，孵育1小時。檢測595 nm/620 nm的吸光值。
實驗圖片	檢測方法	檢測指標	實驗圖片	PMID
	Western blot	ASCT2 / GLS1 c-Myc		25872876
	Growth inhibition assay	Cell viability		25872876

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	Troglitazone是一種有效的抗糖尿病藥，以一種全新的機制發(fā)揮作用。但是，在它被廣泛使用后的幾年內(nèi)，發(fā)現(xiàn)它對一些個體具有肝臟損傷、造成肝功能衰竭^[5]。TGZ顯著抑制攜有HCT-116, MCF-7, PC-3癌細胞的免疫缺陷小鼠的腫瘤生長^[3]。在實驗性慢性胰腺炎模型中，Troglitazone能夠減輕胰腺損傷和炎癥反應^[4]。
動物實驗	Animal Models	C57BL/6小鼠
	Dosages	0.2% (with chow)
	Administration	口服

參考文獻
[1] Park JW, et al. Thyroid. 2005, 15(3):222-31. [2] Bolden A, et al. PPAR Res. 2012, 2012:929052. [3] Baek SJ, et al. J Biol Chem. 2003, 278(8):5845-53. [4] van Westerloo DJ, et al. Am J Pathol. 2005, 166(3):721-8. [5] Jaeschke H. Toxicol Sci. 2007, 97(1):1-3. [6] Sebastian Doll, et al. Nat Chem Biol . 2017 Jan;13(1):91-98. + 展開

參考文獻

[1] Park JW, et al. Thyroid. 2005, 15(3):222-31.
[2] Bolden A, et al. PPAR Res. 2012, 2012:929052.
[3] Baek SJ, et al. J Biol Chem. 2003, 278(8):5845-53.

[4] van Westerloo DJ, et al. Am J Pathol. 2005, 166(3):721-8.
[5] Jaeschke H. Toxicol Sci. 2007, 97(1):1-3.
[6] Sebastian Doll, et al. Nat Chem Biol . 2017 Jan;13(1):91-98.

+ 展開

化學信息&溶解度

分子量	441.54	分子式	C₂₄H₂₇NO₅S
CAS號	97322-87-7	SDF	Download Troglitazone SDF
Smiles	CC1=C(C2=C(CCC(O2)(C)COC3=CC=C(C=C3)CC4C(=O)NC(=O)S4)C(=C1O)C)C
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 88 mg/mL ( (199.3 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 15 mg/mL (33.97 mM)

Water : Insoluble

DMSO : 88 mg/mL ( (199.3 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 6 mg/mL (13.58 mM)

Water : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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