Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 113.00 | |
5 mg | In stock | $ 282.00 | |
10 mg | In stock | $ 448.00 | |
25 mg | In stock | $ 747.00 | |
50 mg | In stock | $ 1,050.00 | |
100 mg | In stock | $ 1,420.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 358.00 |
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. |
Targets&IC50 | Monkey glucocorticoid receptor, cell-based assay:210 nM, Human glucocorticoid receptor, cell-based assay:81.2 nM(ki), Glucocorticoid receptor, cell-based assay:(ki)7.2 nM, Rat glucocorticoid receptor, cell-based assay:12 nM(ki) |
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]. |
Synonyms | CORT 125134 |
Molecular Weight | 586.56 |
Formula | C27H22F4N6O3S |
CAS No. | 1496510-51-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 22.5 mg/mL (38.36 mM)
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Relacorilant 1496510-51-0 Endocrinology/Hormones Glucocorticoid Receptor CORT 125134 CORT-125134 CORT125134 inhibitor inhibit