AZD-7594

AZD7594 is a potent selective nonsteroidal glucocorticoid receptor modulator, with an IC50 of 0.9 nM.

Signaling Pathways >> GPCR/G Protein >> Glucocorticoid Receptor

Research Areas >> Inflammation/Immunology

IC50: 0.9 nM (Glucocorticoid receptor)[1]

AZD7594 is a potent selective nonsteroidal glucocorticoid receptor modulator, with an IC50 of 0.9 nM. AZD7594 shows no effect on progesterone receptor, mineralocorticoid receptor, Androgen receptor, ERα or ERβ (IC50, > 10 μM).

AZD7594 has anti-inflammatory activity, and efficiently inhibits rat lung edema[1].

Androgen receptor (AR) binding is measured in a fluorescence polarization ligand displacement assay using commercially available reagents, including recombinant rat AR ligand binding domain tagged with His and GST, Fluormone labelled AL Green ligand, DTT and AR Green assay buffer (containing protein stabilizing agents and glycerol, pH 7.5). Test compounds (AZD7594, etc.) and controls in 100% DMSO are added to 384-well plates in 0.2 μL. AR-LBD and Fluomone AL Green in AR Green assay buffer are added to 12.5 nM and 0.5 nM in a final volume of 15 μL. Plates are incubated in the dark at room temperature for 4-6 hours before fluorescence polarization is measured (excitation 485 nm, emission 530 nm). The shift in polarization value in the presence of test compounds (AZD7594, etc.) is used to determine relative affinity of test compounds for AR. The minimum and maximum values are determined in the in the presence of testosterone (1.3 μM) and in the absence of test compound. The molar concentration of compound producing 50% binding (IC50) of AR is mesured[1].

[1]. Hemmerling M, et al. Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases. J Med Chem. 2017 Oct 26;60(20):8591-8605.

Hydrocortisone | Mifepristone | Corticosterone | Prednisone | (20S)-Protopanaxatriol | Fluticasone propionate | Triamcinolone | Cortisone | AL 082D06 | Glucocorticoid receptor agonist | Mapracorat | Ciclesonide | Beclometasone dipropionate | Clobetasol propionate | CORT-108297