切换导航

XCT790

现货
Catalog No.
B3238
ERRα激动剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,300.00
现货
10mg
¥ 900.00
现货
50mg
¥ 4,000.00
现货

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Background

XCT790 is an inverse agonist of Estrogen-related receptor alpha (ERRα) with IC50 value of 0.37μM [1].

XCT790 is a first and selective inverse agonist of ERRα. It does not significantly inhibit ERRγ, ERα and ERβ below 10μM. XCT790 is proved to bind ERRα within LBD [1].

As an agonist of ERRα, XCT790 is found to decrease mitochondrial masses as well as affect the mitochondrial membrane potential, results in a subsequent function dysregulation of mitochondrial. XCT790 also reduces the expression level of PGC-1α which is a coactivator of ERRα to regulate mitochondrial biogenesis. Additionally, XCT790 can induce cell death in human hepatocarcinoma cell lines. It reduces the viabilities of HepG2 and its MDR cell line R-HepG2, MES-SA/DX5 and MES-SA in a dose-dependent manner. The mechanism of causing cell death is that XCT790 induces apoptosis through inducing ROS and subsequent caspases activation [2].

References:
[1] Lu X, Peng L, Lv M, ding K. Recent advance in the design of small molecular modulators of estrogen-related receptors. Curr Pharm Des. 2012;18(23):3421-31.
[2] Wu F, Wang J, Wang Y, Kwok TT, Kong SK, Wong C. Estrogen-related receptor alpha (ERRalpha) inverse agonist XCT-790 induces cell death in chemotherapeutic resistant cancer cells. Chem Biol Interact. 2009 Oct 7;181(2):236-42.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt596.42
Cas No.725247-18-7
FormulaC23H13F9N4O3S
Solubility≥14.9mg/mL in DMSO
Chemical Name(E)-3-[4-[[2,4-bis(trifluoromethyl)phenyl]methoxy]-3-methoxyphenyl]-2-cyano-N-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]prop-2-enamide
SDFDownload SDF
Canonical SMILESCOC1=C(C=CC(=C1)C=C(C#N)C(=O)NC2=NN=C(S2)C(F)(F)F)OCC3=C(C=C(C=C3)C(F)(F)F)C(F)(F)F
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 :

细胞系

人乳腺上皮细胞系MCF7,H295R肾上腺皮质癌细胞系

溶解方法

该化合物在DMSO中的溶解度有限。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应时间

1、5、10 μM,1-48小时

应用

XCT790诱导雌激素受体相关受体α(ERRα)失活和蛋白酶体降解。XCT790加强ICI182,780诱导的ERα降解 [1]。此外,XCT790抑制H295R肾上腺皮质癌细胞系的细胞增殖,阻断G1/S转换 [2]。

动物实验 [2]:

动物模型

H295R细胞异种移植肿瘤模型

剂量

2.5 mg/kg,隔天给药,21天;

应用

XCT790减少建立的H295R细胞异种移植肿瘤生长并减少体内H295R细胞增殖。

注意事项

请于室内测试所有化合物的溶解度。实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

1. Lanvin, O., Bianco, S., Kersual, N., Chalbos, D. and Vanacker, J. M. (2007) Potentiation of ICI182,780 (Fulvestrant)-induced estrogen receptor-alpha degradation by the estrogen receptor-related receptor-alpha inverse agonist XCT790. J Biol Chem. 282, 28328-28334

2. Casaburi, I., Avena, P., De Luca, A., Chimento, A., Sirianni, R., Malivindi, R., Rago, V., Fiorillo, M., Domanico, F., Campana, C., Cappello, A. R., Sotgia, F., Lisanti, M. P. and Pezzi, V. (2015) Estrogen related receptor alpha (ERRalpha) a promising target for the therapy of adrenocortical carcinoma (ACC). Oncotarget. 6, 25135-25148

质量控制

化学结构

XCT790