RORγt Inverse agonist 10 is a highly potent and orally bioavailable compound that acts as an antagonist for the retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt). With an IC50 of 51 nM, it effectively inhibits the activity of RORγt, a prominent transcription factor involved in the regulation of genes associated with the pathogenesis of psoriasis, including IL-17A, IL-22, and IL-23R.

RORγt:51 nM (IC50)

RORγt Inverse agonist 10 has a good liver microsome stability (human CL int =0.010 mL/min/mg, mouse CL int =0.030 mL/min/mg)[1]. RORγt Inverse agonist 10 suppresses the IL-17A production in a dose-dependent manner with an IC 50 of 130 nM in a human whole-blood assay[1].

RORγt Inverse agonist 10 (3-100 mg/kg; p.o.) shows robust and dose-dependent inhibitory effect on the IL-17A production in mouse IL-18/23-induced cytokine expression model[1]. RORγt Inverse agonist 10 (1.145 mg/kg; p.o.) shows a high AUC of 15000 nM*h and t 1/2 of 3.6 hours[1]. Animal Model: C57/BL6 male mice, mouse IL-18/23-induced cytokine expression model[1]Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg Administration: Oral administration Result: Significantly inhibited the IL-17A production in a dose-dependent manner. Animal Model: Mice[1]Dosage: 1.145 mg/kg (Pharmacokinetic Analysis) Administration: Oral administration Result: AUC=15000 nM*h, t 1/2 =3.6 hours.