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Submit ReviewXCT 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.
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 5.96 | 10 with gentle warming |
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.
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 |
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.
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
Citations are publications that use Tocris products. Selected citations for XCT 790 include:
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
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
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
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
Do you know of a great paper that uses XCT 790 from Tocris? Please let us know.
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