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XCT790 (CAS 725247-18-7) LS-H122

ERR alpha agonist
LS-H122-1 / 1 mg / $175
LS-H122-5 / 5 mg / $235
LS-H122-10 / 10 mg / $265
USA Shipment Only
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Description: XCT790 is an inverse agonist of estrogen-related receptor alpha (ERR alpha ; IC50 = ~300-500 nM). It demonstrates 90-100% inhibition of ERR alpha constitutive activity and has no significant activity at related nuclear receptors at 10 µM. XCT790 associates with the ligand-binding domain of ERR alpha and blocks ERR alpha /PGC-1 alpha -dependent signaling, suppressing the expression of monoamine oxidases A and B. XCT790 induces proteasomal degradation of ERR alpha and potentiates the degradation of the estrogen receptor ER alpha by fulvestrant . H122_ChemicalStructureImage.png
3-[4-[[2,4-bis(trifluoromethyl)phenyl]methoxy]-3-methoxyphenyl]-2-cyano-N-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]-2-propenamide
 
biochemical, chemical, agonist
LS-H122
725247-18-7
C23H13F9N4O3S
≥98%
A crystalline solid
 
COC1=CC(/C=C(C(NC2=NN=C(C(F)(F)F)S2)=O)\C#N)=CC=C1OCC3=C(C(F)(F)F)C=C(C(F)(F)F)C=C3
InChI=1S/C23H13F9N4O3S/c1-38-17-7-11(6-13(9-33)18(37)34-20-36-35-19(40-20)23(30,31)32)2-5-16(17)39-10-12-3-4-14(21(24,25)26)8-15(12)22(27,28)29/h2-8H,10H2,1H3,(H,34,36,37)/b13-6+
HQFNFOOGGLSBBT-AWNIVKPZSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: ESRRA / ERR Alpha related products

Usage Information

XCT790 is supplied as a crystalline solid. A stock solution may be made by dissolving the XCT790 in the solvent of choice. XCT790 is soluble in organic solvents such as DMSO and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of XCT790 in these solvents is approximately 3 and 12 mg/ml, respectively. XCT790 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, XCT790 should first be dissolved in DMF and then diluted with the aqueous buffer of choice. XCT790 has a solubility of approximately 0.03 mg/ml in a 1:30 solution of DMF:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Busch, B.B., Stevens, W.C., Jr., Martin, R., et al. Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor α J. Med. Chem. 47(23), 5593-5596 (2004).
  2. Willy, P.J., Murray, I.R., Qlan, J., et al. Regulation of PPARγ coactivator 1α (PGC-1α) signaling by an estrogen-related receptor α (ERRα) ligand. Proc. Natl. Acad. Sci. USA 101(24), 8912-8917 (2004).
  3. Lanvin, O., Bianco, S., Kersual, N., et al. Potentiation of ICI182,780 (Fulvestrant)-induced estrogen receptor-α degradation by the estrogen receptor-related receptor-α inverse agonist XCT790. J. Biol. Chem. 282(39), 28328-28334 (2007).

 


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