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)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
5.96
10mM with gentle warming
Preparing Stock Solutions
The following data is based on the product molecular weight 596.42. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
1.68 mL
8.38 mL
16.77 mL
5 mM
0.34 mL
1.68 mL
3.35 mL
10 mM
0.17 mL
0.84 mL
1.68 mL
50 mM
0.03 mL
0.17 mL
0.34 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Lanvinet 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
Konget 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
Willyet 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 PMID: