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XCT790 {[allProObj[0].p_purity_real_show]}

货号:A216057 同义名: Compound 12 Ambeed 开学季,买赠积分,赢豪礼

XCT-790 is an agonist of estrogen related receptor alpha (ERRα) and can induce death of cancer cells resistant to chemotherapy.

XCT790 化学结构 CAS号:725247-18-7
XCT790 化学结构
CAS号:725247-18-7
XCT790 3D分子结构
CAS号:725247-18-7
XCT790 化学结构 CAS号:725247-18-7
XCT790 3D分子结构 CAS号:725247-18-7
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XCT790 纯度/质量文件 产品仅供科研

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XCT790 生物活性

描述 The estrogen-related receptor α (ERRα) is an orphan nuclear receptor that can be regulated by peroxisome proliferator-activated receptor γ coactivator-1 (PGC-1). XCT790 is a selective inverse agonist for ERRα with an IC50 value of 0.37 μM, but displays no activity against ERRγ and estrogen receptors ERα and ERβ[3]. XCT-790 at 5 – 20 μM reduced the viability of HepG2 and R-HepG2 cells in a dose-dependent manner. The treatment of HepG2 and R-HepG2 cells with XCT-790 (10 μM) for 24 h reduced the protein levels of ERRα and decreased mitochondrial masses as compared to the DMSO-treated control group[4]. In mice inoculated with H295R adrenocortical cancer cells, the administration of XCT790 (2.5 mg/kg) for 21 days decreased H295R cell proliferation and suppressed tumor growth compared to the vehicle-treated group[5].
作用机制 XCT790 is a thiadiazoleacrylamide that functions as a potent inverse agonist of ERRα[3].

XCT790 参考文献

[1]Wu F, Wang J, et al. 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.

[2]Busch BB, Stevens WC Jr, et al. Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor alpha. J Med Chem. 2004 Nov 4;47(23):5593-6.

[3]Busch BB, Stevens WC Jr, Martin R, et al. Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor alpha. J Med Chem. 2004;47(23):5593-5596. doi:10.1021/jm049334f

[4]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;181(2):236-242. doi:10.1016/j.cbi.2009.05.008

[5]Casaburi I, Avena P, De Luca A, et al. Estrogen related receptor α (ERRα) a promising target for the therapy of adrenocortical carcinoma (ACC). Oncotarget. 2015;6(28):25135-25148. doi:10.18632/oncotarget.4722

XCT790 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.68mL

0.34mL

0.17mL

8.38mL

1.68mL

0.84mL

16.77mL

3.35mL

1.68mL

XCT790 技术信息

CAS号725247-18-7
分子式C23H13F9N4O3S
分子量 596.425
别名 Compound 12
运输蓝冰
存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 16 mg/mL(26.83 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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