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 conditions.
性状
Solid
IC50 & Target[1][2]
RORγt
体外研究(In Vitro)
JNJ-61803534 在转染了编码 RORγt 载体的 HEK-293 T 细胞中抑制 RORγt 转录,IC50 为 9.6 nM。 JNJ-61803534 (1 nM-1 μM) 抑制人血液中分离的 CD4+ T 细胞产生 IL-17A、IL-17F IFNγ 和 IL-22。JNJ-61803534 不影响 CD4+ T 细胞的体外 Treg 分化。 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
JNJ-61803534 (100 mg/kg,口服) 抑制小鼠血液中体外刺激产生的 IL-17A。
JNJ-61803534 (3-100 mg/kg BID 或 60 mg/kg QD,p.o.) 减轻小鼠胶原诱导性关节炎 (CIA) 模型的炎症、软骨损伤和骨质破坏。
JNJ-61803534 (30 和 100 mg/kg,口服) 减轻小鼠 Imiquimod (HY-B0180) 诱导的皮肤银屑病样炎症。 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Mod
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Xue X, et al. Preclinical and clinical characterization of the RORγt inhibitor JNJ-61803534. Sci Rep. 2021 May 26;11(1):11066.
溶解度数据
In Vitro: DMSO : 300 mg/mL (482.00 mM; Need ultrasonic)配制储备液