1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Immunology/Inflammation
  2. ROR Interleukin Related
  3. A-9758

A-9758 是一种 RORγ 配体和一种有效选择性的 RORγt 反向激动剂 (IC50 值为 5 nM),并且强效抑制 IL-17A 释放。A-9758 有效抑制 Th17 分化和 Th17 效应子功能。A-9758 显着减弱 IL-23 驱动型银屑病性皮炎,并有效阻断皮肤和关节炎症。

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A-9758 Chemical Structure

A-9758 Chemical Structure

CAS No. : 2055271-22-0

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生物活性

A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC50=5 nM), and exhibits robust potency against IL-17A release. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis and is effective in blocking skin and joint inflammation[1].

IC50 & Target[1]

RORγt

5 nM (IC50)

IL-17A

 

IL-23

 

体外研究
(In Vitro)

A-9758 inhibits human, mouse, dog and rat RORγ transactivation (IC50=38 nM, 20 nM, 25 nM and 64 nM, respectively)[1].
A-9758 displays a cofactor profile in recruiting co-repressors (NCoR1: EC50=60 nM, NCoR2: EC50=43 nM) and derecruiting co-activators (NCoA1: IC50=110 nM, PGC1α: IC50=49 nM)[1].
A-9758 inhibits TCR-mediated IL-17A secretion with an IC50 of 100 and 38 nM for human CD4+ T cells and in vitro differentiated mouse Th17 cells, respectively. A-9758 attenuates the differentiation of RORγt expressing Th17 cells and/or their effector function[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

527.36

Formula

C25H23Cl2F3N2O3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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A-9758
目录号:
HY-126252
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