Preferred Label : Relacorilant;
NCIt synonyms : Methanone, ((4aR)-1-(4-Fluorophenyl)-1,4,5,6,7,8-hexahydro-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4aH-pyrazolo(3,4-g)isoquinolin-4a-yl)(4-(trifluoromethyl)-2-pyridinyl)-; ((4aR)-1-(4-Fluorophenyl)-6-(1-methyl-1H-pyrazole-4-sulfonyl)-1,4,5,6,7,8-hexahydro-4aH-pyrazolo(3,4-g)isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone;
NCIt definition : An orally available antagonist of the glucocorticoid receptor (GR), with potential
antineoplastic activity. Upon administration, relacorilant competitively binds to
and blocks GRs. This inhibits the activity of GRs, and prevents both the translocation
of the ligand-GR complexes to the nucleus and gene expression of GR-associated genes.
This decreases the negative effects that result from excess levels of endogenous glucocorticoids,
like those seen when tumors overproduce glucocorticoids. In addition, by binding to
GRs and preventing their activity, inhibition with CORT125134 also inhibits the proliferation
of GR-overexpressing cancer cells. GRs are overexpressed in certain tumor cell types
and promote tumor cell proliferation.;
UNII : 2158753C7E;
InChIKey : WANIDIGFXJFFEL-SANMLTNESA-N;
CAS number : 1496510-51-0;
Molecule name : CORT-125134;
NCI Metathesaurus CUI : CL507918;
Origin ID : C127838;
UMLS CUI : C4743554;
Automatic exact mappings (from CISMeF team)
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
