A selective inverse agonist of ERRα (IC50 = ~300-500 nM); blocks ERRα/PGC-1α-dependent signaling

XCT790 – 5 mg

Brand:
Cayman
CAS:
725247-18-7
Storage:
-20
UN-No:
Non-Hazardous - /

XCT790 is an inverse agonist of estrogen-related receptor α (ERRα; IC50 = ~300-500 nM).{31192,31194} It demonstrates 90-100% inhibition of ERRα constitutive activity and has no significant activity at related nuclear receptors at 10 µM.{31194} 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.{31194} XCT790 induces proteasomal degradation of ERRα and potentiates the degradation of the estrogen receptor ERα by fulvestrant (Item No. 10011269).{31193}  

 

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Description

A selective inverse agonist of ERRα (IC50 = ~300-500 nM); blocks ERRα/PGC-1α-dependent signaling, suppressing the expression of MAO A and B; induces proteasomal degradation of ERRα and potentiates the degradation of ERα by fulvestrant

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

Synonyms: 

Molecular weight: 596.4

CAS: 725247-18-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Inverse Agonists||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins

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