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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-ROR-JNJ-61803534
JNJ-61803534

Chemical Structure : JNJ-61803534

CAS No.: 1917306-14-9

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JNJ-61803534 (JNJ 61803534)

货号: PC-72400Not For Human Use, Lab Use Only.

JNJ-61803534 (JNJ 61803534) is a novel, selective and potent RORγt inverse agonist, inhibits RORγt-driven transcription with IC50 of 9.6 nM in 1-hybrid reporter assays.

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2 mg ￥3580 In stock
5 mg ￥5980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

JNJ-61803534 (JNJ 61803534) is a novel, selective and potent RORγt inverse agonist, inhibits RORγt-driven transcription with IC50 of 9.6 nM in 1-hybrid reporter assays.
JNJ-61803534 demonstrated high selectivity for RORγt over RORα and RORβ (IC50>2 uM), as well as against 18 human nuclear receptors and a panel of 52 receptors, ion channels and transporters, 28 GPCRs.
JNJ-61803534 dose-dependently suppressed production of IL-17A, IL-17F and IL-22 with IC50 values of 19nM, 22 nM and 27 nM, respectively, in human CD4+ T cells under Th17 differentiation, does not impair human nTreg suppressive function.
JNJ-61803534 specifically blocked RORγt-dependent pathways in cellular assays and significantly reduced inflammation in preclinical models.

物理化学性质&存储条件

分子量 622.404
分子式 C23H23Cl2F6N3O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

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]-

参考文献

1. Xiaohua Xue, et al. Sci Rep. 2021 May 26;11(1):11066.

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