XCT 790

Pricing Availability   Qty
Description: Selective ERRα inverse agonist
Chemical Name: 3-[4-(2,4-Bis-trifluoromethylbenzyloxy)-3-methoxyphenyl]-2-cyano-N-(5-trifluoromethyl-1,3,4-thiadiazol-2-yl)acrylamide
Purity: ≥99% (HPLC)
Datasheet
Citations (4)
Reviews
Pathways (1)

Biological Activity for XCT 790

XCT 790 is a selective ERRα inverse agonist (IC50 = ~400 nM). Displays no antagonist activity at ERRγ or ERα at concentrations below 10 μM. Interferes with PPARγ coactivator-1α (PGC-1α)/ERRα-dependent signaling: inhibits PGC-1α induction of ERRα and MAO-B gene expression and downregulates the constitutive transcriptional activity of ERRα in numerous cell lines.

Technical Data for XCT 790

M. Wt 596.42
Formula C23H13F9N4O3S
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 725247-18-7
PubChem ID 6918788
InChI Key HQFNFOOGGLSBBT-AWNIVKPZSA-N
Smiles O=C(NC3=NN=C(C(F)(F)F)S3)/C(C#N)=C/C(C=C2OC)=CC=C2OCC1=C(C(F)(F)F)C=C(C(F)(F)F)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for XCT 790

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 5.96 10 with gentle warming

Preparing Stock Solutions for XCT 790

The following data is based on the product molecular weight 596.42. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 16.77 mL 83.83 mL 167.67 mL
0.5 mM 3.35 mL 16.77 mL 33.53 mL
1 mM 1.68 mL 8.38 mL 16.77 mL
5 mM 0.34 mL 1.68 mL 3.35 mL

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References for XCT 790

References are publications that support the biological activity of the product.

Lanvin et al (2007) Potentiation of ICI182,780 (Fulvestrant)-induced estrogen receptor-alpha degradation by the estrogen receptor-related receptor-α inverse agonist XCT790. J.Biol.Chem. 282 28328 PMID: 17631492

Kong et al (2009) Peroxisome proliferator-activated receptor γ coactivator-1α enhances antiproliferative activity of 5'-deoxy-5-fluorouridine in cancer cells through induction of uridine phosphorylase. Mol.Pharmacol. 76 854 PMID: 19602572

Willy et al (2004) Regulation of PPARγ coactivator 1α (PGC-1α) signaling by an estrogen-related receptor alpha (ERRα) ligand. Proc.Natl.Acad.Sci.USA 101 8912

Theodoris et al (2021) Network-based screen in iPSC-derived cells reveals therapeutic candidate for heart valve disease. Science. 371 PMID: 33303684


If you know of a relevant reference for XCT 790, please let us know.

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Keywords: XCT 790, XCT 790 supplier, XCT790, ERRalpha, ERRa, ERRα, antagonists, inverse, agonists, PPARγ, PPARg, PPARgamma, coactivator-1α, coactivator-1alpha, coactivator-1a, PGC-1α, PGC-1alpha, PGC-1a, signaling, signalling, Estrogen, and, Related, Receptors, 3928, Tocris Bioscience

4 Citations for XCT 790

Citations are publications that use Tocris products. Selected citations for XCT 790 include:

Núria et al (2021) The Nuclear Receptor ESRRA Protects from Kidney Disease by Coupling Metabolism and Differentiation. Cell Metab 33 379-394.e8 PMID: 33301705

Teng et al (2014) Development of a stable cell line with an intact PGC-1α/ERRα axis for screening environmental chemicals. Mol Cancer 444 177 PMID: 24457025

Hwang et al (2014) Estrogen-related receptor α is required for efficient human cytomegalovirus replication. Proc Natl Acad Sci U S A 111 E5706 PMID: 25512541

Michael P et al (2015) Estrogen related receptor α (ERRα) a promising target for the therapy of adrenocortical carcinoma (ACC). Oncotarget 6 25135-48 PMID: 26312764


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Pathways for XCT 790

Estrogen Signaling Pathway

Estrogen Signaling Pathway

Estrogen is a steroid hormone that is responsible for the regulation of growth, differentiation and function of the reproductive system. Estrogen signaling is often dysregulated in breast cancer and osteoporosis.