RORγt Inverse agonist 10

RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC 50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A , IL-22 , and IL-23R In Vitro 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). 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57/BL6 male mice, mouse IL-18/23-induced cytokine expression model 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 Dosage: 1.145 mg/kg (Pharmacokinetic Analysis) Administration: Oral administration Result: AUC=15000 nM*h, t 1/2 =3.6 hours. Form:Solid IC50& Target:RORγt 51 nM (IC 50 )

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