cushing's

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.

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.

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.

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

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.

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.