Glucocorticoid receptor modulator 1 is a highly potent and orally active non-steroidal selective glucocorticoid receptor modulator with an IC50 value of 9 nM and 130 nM for NF-κB and AP-1, respectively. Glucocorticoid receptor modulator 1 can effectively reduce the expression of inflammatory factors IL-6, IL-1β, TNF-α, also can relieve dermatitis in mice.
Glucocorticoid receptor modulator 1 (compound B53) shows inhibitory activities against NF-κB and AP-1 with IC50s of 9 nM and 130 nM, respectively[1].
Glucocorticoid receptor modulator 1 (10 μM; 24 h) decreases the mRNA expression of the inflammatory factors of IL-6, IL-1β, TSLP, MMP-13, TNF-α, and CCL-2[1].
Glucocorticoid receptor modulator 1 (5, 10 and 20 mg/kg; p.o.; for 24 days) relieves dermatitis in mice and suppresses the expression of inflammatory factors[1].
References:
[1]. Li D, Hou T, et al. Discovery and Optimization of N-Acyl-6-sulfonamide-tetrahydroquinoline Derivatives as Novel Non-Steroidal Selective Glucocorticoid Receptor Modulators. J Med Chem. 2022 Nov 18.