cushing's

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.

Pasireotide (SOM230) acetate is a long-acting cyclohexapeptide growth hormone inhibitory hormone analog with antisecretory, antiproliferative, and proapoptotic activities.Pasireotide (SOM230) acetate inhibits the secretion of GH, IGF-I, and ACTH, and can be used in the study of acromegaly and Cushing's disease. Pasireotide (SOM230) acetate also enhances the agonist activity of growth inhibitory receptors, with pKi of 8.2, 9.0, 9.1, <7.0 and 9.9 for sst1, 2, 3, 4 and 5, respectively.

Metyrapone (NSC-25265) is an inhibitor of the enzyme STEROID 11-BETA-MONOOXYGENASE. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of CUSHING SYNDROME.

Roridin A (Roridine A), a compound isolated from Verruca sp., showed nematicidal activity against Meloidogyne incognita.Roridin A is cytotoxic and has immunomodulatory activity.Roridin A has been used in the study of adrenocortical hyperplasia (CAH) and Cushing's disease (CD).

11-Beta-hydroxyandrostenedione (NSC-17102) is a steroid mainly found in the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue), which is a 11β-hydroxysteroid dehydrogenase isozymes inhibitor. Measuring plasma 11-Beta-hydroxyandrostenedione can distinguish the adrenal or ovarian origin of hyperandrogenism with 4-androstenedione increases.

SPI-09 (also known as ASP5309) is an HSD-1 inhibitor, showing promise as a potential new treatment for endogenous Cushing's syndrome.

Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase (CYP11B1) and aldosterone synthase (CYP11B2) with IC50 values ​​of 2.5 and 0.7 nM, respectively, and has been approved by the FDA for the treatment of Cushing's disease.

Atumelnant (CRN04894) is a selective and potent MC2R antagonist that inhibits ACTH-stimulated corticosterone secretion in a dose-dependent manner for the study of congenital adrenocortical hyperplasia (CAH) and Cushing's disease (CD).

Trilostane-d3 is a deuterium-substituted isotope-labeled compound of Trilostane, which is used primarily as a quantitative tracer.Trilostane is a competitive and specific inhibitor of 3-beta-hydroxysteroid dehydrogenase (3β-HSD), with the advantage of oral activity.Trilostane reduces the synthesis of steroid hormones by inhibiting the activity of 3β-HSD, and can be Used in studies of Cushing's syndrome (hypercortisolism), Con's syndrome (hyperaldosteronism), and postmenopausal breast cancer.