| Description |
Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively; Relacorilant has entered phase 2 clinical study in patients with Cushing’s syndrome.
|
| Related Catalog |
|
| Target |
Ki: 7.2 nM (Glucocorticoid receptor, cell-based assay), 12 nM (Rat glucocorticoid receptor, cell-based assay), 81.2 nM (Human glucocorticoid receptor, cell-based assay), 210 nM (Monkey glucocorticoid receptor, cell-based assay)[1]
|
| In Vitro |
Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively. Relacorilant also shows potent inhibition on CYP2C8 and CYP3A4 (IC50s, 0.21, 1.3 μM, respectively), modestly inhibits CYP2C9, 2C19, 2D6 and 3A5, with ICC50s of 2, 8, 9, and 4.9 μM, respectively[1].
|
| In Vivo |
Relacorilant (30 mg/kg, p.o., twice a day) dramaticlly blocks the effects on plasma insulin and completely inhibits cortisone induced increase in plasma glucose in rats of exogenous Cushing’s syndrome, and similar effect is also observed when administrated with of Relacorilant at 7.5 mg/kg twice a day[1].
|
| References |
[1]. Hunt HJ, et al. Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist. J Med Chem. 2017 Apr 27;60(8):3405-3421.
|
