RORγt inverse agonist 13

RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved agent-like properties, with an IC 50 of 63.8 nM In Vitro RORγt inverse agonist 13 (Compound 3i) exhibits activity with an inhibition of 76% at 0.3 µM in Th17 cell differentiation assay. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo RORγt inverse agonist 13 (Compound 3i, 25 mg/kg, Orally, twice daily) demonstrats excellent in vivo PK profile in mice and good in vivo efficacy in an IMQ-induced psoriasis mice model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Imiquimod (IMQ)-induced psoriasis mice model . Dosage: 25 mg/kg. Administration: Orally, twice daily. Result: Brought in a significant reduction in clinical severity of psoriasis as measured through the ear erythema, back skin erythema and scaliness scales. Animal Model: Male CD-1 Mice . Dosage: 1 mg/kg (i.v.) and 5 mg/kg (p.o.)(Pharmacokinetic Analysis). Administration: IV or PO, single dose. Result: C max : 609.67 ng/mL (PO), 1550 ng/mL (IV). T 1/2 : 3.63 h (PO), 3.04 h (IV). Form:Solid IC50& Target:ROR-γ 63.8 nM (IC 50 )

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