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XCT 790

Cat No. 3928

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Chemical Name: 3-[4-(2,4-Bis-trifluoromethylbenzyloxy)-3-methoxyphenyl ]-2-cyano-N-(5-trifluoromethyl-1,3,4-thiadiazol-2-yl)ac rylamide

Biological Activity

Selective ERRα antagonist/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

M.Wt:

596.42

Formula:

C₂₃H₁₃F₉N₄O₃S

Solubility:

Soluble to 25 mM in DMSO

Purity:

>99 %

Storage:

Store at +4°C

CAS No:

[725247-18-7]

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

Resources

Certificate of Analysis / MSDS

Certificate of Analysis: View current batch

Material Safety Data Sheet: View current batch

References

Willy et al (2004) Regulation of PPARgamma coactivator 1alpha (PGC-1alpha) signaling by an estrogen-related receptor alpha (ERRalpha) ligand. Proc.Natl.Acad.Sci.USA 101 8912. Lanvin et al (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. Kong et al (2009) Peroxisome proliferator-activated receptor gamma coactivator-1alpha enhances antiproliferative activity of 5'-deoxy-5-fluorouridine in cancer cells through induction of uridine phosphorylase. Mol.Pharmacol. 76 854.

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Estrogen Receptors

Keywords: XCT 790, XCT790, ERRalpha, ERRa, ERRα, antagonists, inverse, agonists, PPARγ, PPARg, PPARgamma, coactivator-1α, coactivator-1alpha, coactivator-1a, PGC-1α, PGC-1alpha, PGC-1a, signaling, signalling