产品说明书

XCT790

Print
Chemical Structure| 725247-18-7 同义名 : Compound 12
CAS号 : 725247-18-7
货号 : A216057
分子式 : C23H13F9N4O3S
纯度 : 99%+
分子量 : 596.425
MDL号 : MFCD08277031
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：
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].
实验方案
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
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