For research use only. Not for therapeutic Use.
JNJ-61803534 is a potent and orally active RORγt inverse agonist with an IC50 of 9.6 nM. JNJ-61803534 has anti-inflammatory activity. JNJ-61803534 inhibits IL-17A production in human CD4+ T cells under Th17 differentiation conditions[1].
JNJ-61803534 inhibits RORγt transcription in HEK-293 T cells transfected with vectors encoding RORγt, with an IC50 of 9.6 nM[1].
JNJ-61803534 (1 nM-1 μM) inhibits IL-17A, IL-17F IFNγ and IL-22 production in CD4+ T cells isolated from human blood[1].
JNJ-61803534 does not impact in vitro Treg differentiation in CD4+ T cells[1].
JNJ-61803534 (100 mg/kg, p.o.) inhibits ex vivo stimulated IL-17A production in the blood of mice[1].
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[1].
JNJ-61803534 (30 and 100 mg/kg, p.o.) alleviates Imiquimod (HY-B0180)-induced dermal psoriatic-like inflammation in mice[1].
Catalog Number | I041787 |
CAS Number | 1917306-14-9 |
Synonyms | 5-[2,3-dichloro-4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-N-(2-hydroxy-2-methylpropyl)-4-[(2R)-2-methylpyrrolidine-1-carbonyl]-1,3-thiazole-2-carboxamide |
Molecular Formula | C23H23Cl2F6N3O4S |
Purity | ≥95% |
InChI | InChI=1S/C23H23Cl2F6N3O4S/c1-10-5-4-8-34(10)19(36)15-16(39-18(33-15)17(35)32-9-20(2,3)37)11-6-7-12(14(25)13(11)24)21(38,22(26,27)28)23(29,30)31/h6-7,10,37-38H,4-5,8-9H2,1-3H3,(H,32,35)/t10-/m1/s1 |
InChIKey | ZQHVEGQHOKDZEN-SNVBAGLBSA-N |
SMILES | CC1CCCN1C(=O)C2=C(SC(=N2)C(=O)NCC(C)(C)O)C3=C(C(=C(C=C3)C(C(F)(F)F)(C(F)(F)F)O)Cl)Cl |
Reference | [1]. Xue X, et al. Preclinical and clinical characterization of the RORγt inhibitor JNJ-61803534. Sci Rep. 2021 May 26;11(1):11066. |