Relacorilant 是一种选择性和口服生物可利用的糖皮质激素受体拮抗剂（HepG2 TAT 试验中的 Kis 为 7.2 nM，在基于细胞的试验中对大鼠、人和猴糖皮质激素受体的 Kis 分别为 12、81.2、210 nM）。 它具有治疗库欣综合征的潜力。

Relacorilant is a selective and orally bioavailable antagonist of glucocorticoid receptor(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 the potential for Cushing’s syndrome treatment.

Relacorilant also displays effective inhibition on CYP2C8 and CYP3A4 (IC50s, 0.21, 1.3 μM, respectively). It also modestly inhibits CYP2C9, 2C19, 2D6, and 3A5 (ICC50s: 2, 8, 9, and 4.9 μM, respectively)[1].

Relacorilant (30 mg/kg, p.o., twice a day) obviously blocks the effects on plasma insulin. It fully inhibits cortisone induced increase in plasma glucose in rats of exogenous Cushing’s syndrome, and a similar effect is also observed when administrated with of Relacorilant at 7.5 mg/kg twice a day [1].

1496510-51-0

C27H22F4N6O3S

586.56

CORT 125134

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years