CP-394531

CP-394531 is an efficient and highly selective non-steroidal glucocorticoid receptor (GR) antagonist, with a Ki value of 0.1 nM. CP-394531 has a weak binding to androgen receptor (AR) (Ki = 130 nM), and has almost no effect on progesterone receptor (PR) and estrogen receptors (ERα, ERβ) . CP-394531 completely blocks the half-maximal agonistic effect induced by Dexamethasone (HY-14648G), with a Kif of 4.1 nM. CP-394531 can be used to study various diseases such as diabetes, obesity, depression, neurodegenerative diseases, glaucoma and Cushing's disease[1].

Product Specifications

CAS Number

[305822-63-3]

UNSPSC

12352005

Target

Androgen Receptor; Glucocorticoid Receptor

Related Pathways

Immunology/Inflammation; Vitamin D Related/Nuclear Receptor

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Neurological Disease; Metabolic Disease

Smiles

O[C@@]1(C#CCl)C[C@@]2([H])CCC3=C(C=CC(O)=C3)[C@]2(CC4=CC=CC=C4)CC1

Molecular Formula

C23H23ClO2

Molecular Weight

366.88

References & Citations

[1]Morgan BP, et al. Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists. J Med Chem. 2002 Jun 6;45 (12) :2417-24.