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Relacorilant
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.
Catalog No. T16727Cas No. 1496510-51-0
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Purity:99%
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Relacorilant
Catalog No. T16727Alias CORT 125134Cas No. 1496510-51-0
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.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $113 | In Stock | |
| 5 mg | $282 | In Stock | |
| 10 mg | $448 | In Stock | |
| 25 mg | $747 | In Stock | |
| 50 mg | $1,050 | In Stock | |
| 100 mg | $1,420 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $358 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
| 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 | GR (monkey, cell-based assay):210 nM, GR (human, cell-based assay):81.2 nM(ki), GR (cell-based assay):(ki)7.2 nM, GR (rat, 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]. |
| Alias | CORT 125134 |
| Molecular Weight | 586.56 |
| Formula | C27H22F4N6O3S |
| Cas No. | 1496510-51-0 |
Storage & Solubility Information
| 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)  | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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