JNJ-61803534 (C09-1140-962)

JNJ-61803534 is a potent and orally active RORγt inverse agonist with an IC 50 of 9.6  nM. JNJ-61803534 has anti-inflammatory activity. JNJ-61803534 inhibits IL-17A production in human CD4+ T cells under Th17 differentiation conditionsIn VitroJNJ-61803534 inhibits RORγt transcription in HEK-293 T cells transfected with vectors encoding RORγt, with an IC 50 of 9.6  nM. JNJ-61803534 (1 nM-1 μM) inhibits IL-17A, IL-17F IFNγ and IL-22 production in CD4+ T cells isolated from human blood. JNJ-61803534 does not impact in vitro Treg differentiation in CD4+ T cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoJNJ-61803534 (100 mg/kg, p.o.) inhibits ex vivo stimulated IL-17A production in the blood of mice . JNJ-61803534 (3-100 mg/kg BID or 60 mg/kg QD, p.o.) alleviates inflammation, cartilage damage, bone destruction in mouse collagen-induced arthritis (CIA) model . JNJ-61803534 (30 and 100 mg/kg, p.o.) alleviates Imiquimod (HY-B0180)-induced dermal psoriatic-like inflammation in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mouse collagen-induced arthritis (CIA) model Dosage: 3-100 mg/kg BID or 60 mg/kg QD Administration: Oral administration (p.o.) Result: Decreased clinical arthritis scores and hind paw histopathology scores.Form:SolidIC50& Target:RORγt. Specification: 0.99 Molecular Formula: C23H23Cl2F6N3O4S Molecular Weight: 622.41