| Name | Relacorilant |
| Description | 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. |
| In vitro | 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]. |
| In vivo | 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 22.5 mg/mL (38.36 mM)
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| Keywords | Relacorilant | CORT-125134 | CORT125134 |
| Inhibitors Related | Nimodipine | Hydrocortisone | Mifepristone | Prednisolone acetate | Beclometasone | Cortisone | Dexamethasone acetate | Prednisolone | Dexamethasone Phosphate disodium | Prednisone acetate | Desonide | Corticosterone |
| Related Compound Libraries | Nuclear Receptor Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
