1. GPCR/G Protein
  2. Glucocorticoid Receptor

Relacorilant (Synonyms: CORT 125134)

Cat. No.: HY-109042
Handling Instructions

Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a 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 entered phase 2 clinical study in patients with Cushing’s syndrome.

For research use only. We do not sell to patients.

Relacorilant Chemical Structure

Relacorilant Chemical Structure

CAS No. : 1496510-51-0

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  • Biological Activity

  • Technical Information

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Description

Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a 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 entered phase 2 clinical study in patients with Cushing’s syndrome.

IC50 & Target

Ki: 7.2 nM (Glucocorticoid receptor, cell-based assay), 12 nM (Rat glucocorticoid receptor, cell-based assay), 81.2 nM (Human glucocorticoid receptor, cell-based assay), 210 nM (Monkey glucocorticoid receptor, cell-based assay)[1]

In Vitro

Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a 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 also shows potent inhibition on CYP2C8 and CYP3A4 (IC50s, 0.21, 1.3 μM, respectively), modestly inhibits CYP2C9, 2C19, 2D6 and 3A5, with ICC50s of 2, 8, 9, and 4.9 μM, respectively[1].

In Vivo

Relacorilant (30 mg/kg, p.o., twice a day) dramaticlly blocks the effects on plasma insulin and completely inhibits cortisone induced increase in plasma glucose in rats of exogenous Cushing’s syndrome, and similar effect is also observed when administrated with of Relacorilant at 7.5 mg/kg twice a day[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7049 mL 8.5243 mL 17.0486 mL
5 mM 0.3410 mL 1.7049 mL 3.4097 mL
10 mM 0.1705 mL 0.8524 mL 1.7049 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

586.56

Formula

C₂₇H₂₂F₄N₆O₃S

CAS No.

1496510-51-0

SMILES

O=C(C1=CC(C(F)(F)F)=CC=N1)[[email protected]@]2(CN(S(=O)(C3=CN(C)N=C3)=O)CC4)C4=CC5=C(C=NN5C6=CC=C(F)C=C6)C2

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Relacorilant
Cat. No.:
HY-109042
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Relacorilant

Cat. No.: HY-109042