| Identification | Back Directory | [Name]
2-Thiazolecarboxamide, 5-[2,3-dichloro-4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-N-(2-hydroxy-2-methylpropyl)-4-[[(2R)-2-methyl-1-pyrrolidinyl]carbonyl]- | [CAS]
1917306-14-9 | [Synonyms]
tert-butyl (3R
4R)-3-fluoro-4-hydroxypiperidine-1-carboxylate
2-Thiazolecarboxamide, 5-[2,3-dichloro-4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-N-(2-hydroxy-2-methylpropyl)-4-[[(2R)-2-methyl-1-pyrrolidinyl]carbonyl]- | [Molecular Formula]
C23H23Cl2F6N3O4S | [MOL File]
1917306-14-9.mol | [Molecular Weight]
622.41 |
| Hazard Information | Back Directory | [Description]
JNJ-61803534 is a novel potent RORγt inverse agonist, selectively inhibiting RORγt-driven transcription versus closely-related family members, RORα and RORβ, also inhibiting IL-17A production in human CD4+ T cells under Th17 differentiation conditions, but not inhibiting IFNγ production under Th1 differentiation conditions, and having neither impact on in vitro differentiation of regulatory T cells (Treg), nor on the suppressive activity of natural Tregs. | [Uses]
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]. | [in vivo]
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].
| Animal Model: | Mouse collagen-induced arthritis (CIA) model[1] | | 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. |
| [IC 50]
RORγt | [References]
[1] Xue X, et al. Preclinical and clinical characterization of the RORγt inhibitor JNJ-61803534. Sci Rep. 2021 May 26;11(1):11066. DOI:10.1038/s41598-021-90497-9 |
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