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XCT790

XCT790

Catalog No.

B3238

ERRα agonist

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Grouped product items
Size	Price	Stock
10mM (in 1mL DMSO)	$105.00	In stock
10mg	$99.00	In stock
50mg	$440.00	In stock

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Background
Chemical Properties
Protocol
Quality Control

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 Appearance	A solid
Storage	Store at -20°C
M.Wt	596.42
Cas No.	725247-18-7
Formula	C₂₃H₁₃F₉N₄O₃S
Solubility	insoluble in H2O; ≥14.9 mg/mL in DMSO; insoluble in EtOH
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
SDF	Download SDF
Canonical SMILES	COC1=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
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment :
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 experiment [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.
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