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XCT790
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
XCT790图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议

产品介绍
XCT-790 是一种有效的选择性 ERRα 反向激动剂,IC50 值为 0.37 μM。 XCT-790 在化疗耐药的癌细胞中诱导细胞死亡。 XCT-790 (Compound 12) 对 ERRγ 和雌激素受体 ERα 和 ERβ 无活性。

Cell lines

The human mammary epithelial cell line MCF7, H295R adrenocortical cancer cell line

Preparation method

The solubility of this compound in DMSO is limited. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1, 5, 10 μM for 1-48 h

Applications

XCT790 induced deactivation and proteasome degradation of estrogen receptor-related receptor-α(ERRα). XCT790 potentiated the ICI182,780-induced ERα degradation [1]. Moreover, XCT790 inhibited the proliferation and blocked G1/S transition of H295R adrenocortical cancer cell line [2].

Animal models

H295R cell xenograft tumors model

Dosage form

2.5 mg/kg, every other day for 21 days;

Applications

XCT790 reduced established H295R cell xenograft tumors growth and decreased H295R cells proliferation in vivo.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

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.