A selective inverse agonist of ERRα
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XCT790

Item No. 16035

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[4-[[2,4-bis(trifluoromethyl)phenyl]methoxy]-3-methoxyphenyl]-2-cyano-N-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]-2-propenamide
CAS Number
725247-18-7
Molecular Formula
C23H13F9N4O3S
Formula Weight
596.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 12 mg/mlDMF:PBS (pH7.2) (1:30): 0.03 mg/mlDMSO: 3 mg/ml
λmax
253, 370 nm
SMILES
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 Code
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+
InChi Key
HQFNFOOGGLSBBT-AWNIVKPZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    Product Description

    XCT790 is an inverse agonist of estrogen-related receptor α (ERRα; IC50 = ~300-500 nM).1,2 It demonstrates 90-100% inhibition of ERRα constitutive activity and has no significant activity at related nuclear receptors at 10 µM.2 XCT790 associates with the ligand-binding domain of ERRα and blocks ERRα/PGC-1α-dependent signaling, suppressing the expression of monoamine oxidases A and B.2 XCT790 induces proteasomal degradation of ERRα and potentiates the degradation of the estrogen receptor ERα by fulvestrant (Item No. 10011269).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description 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. The Journal of Biological Chemisty 282(39), 28328-28334 (2007).