Relacorilant
Product Specifications
CAS Number
1496510-51-0
UNSPSC 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 the potential for Cushing’s syndrome treatment.
Target Antigen
Glucocorticoid Receptor
Type
Reference compound
Related Pathways
Immunology/Inflammation;Vitamin D Related/Nuclear Receptor
Applications
Metabolism-sugar/lipid metabolism
Field of Research
Cardiovascular Disease; Endocrinology
Assay Protocol
https://www.medchemexpress.com/Relacorilant.html
Purity
99.37
Solubility
DMSO : 100 mg/mL (ultrasonic;warming;heat to 60°C)
Smiles
O=C(C1=CC(C(F)(F)F)=CC=N1)[C@@]2(CN(S(=O)(C3=CN(C)N=C3)=O)CC4)C4=CC5=C(C=NN5C6=CC=C(F)C=C6)C2
Molecular Weight
586.56
References & Citations
[1]Hunt HJ, et al. Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist. J Med Chem. 2017 Apr 27;60(8):3405-3421.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Clinical Information
Phase 3
Available Sizes
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