同义名 :	Compound 12
	CAS号 :	725247-18-7
	货号 :	A216057
	分子式 :	C23H13F9N4O3S
	纯度 :	99%+
	分子量 :	596.42
	MDL号 :	MFCD08277031
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	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