Product Introduction
Bioactivity


英文名: A-9758

描述: A-9758 is a RORγ ligand and a selective RORγt inverse agonist (IC50: 5 nM) and exhibits robust potency against IL-17A release. It is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis.

体外活性: A-9758 inhibits human, mouse, dog and rat RORγ transactivation (IC50s: 38 nM, 20 nM, 25 nM and 64 nM). 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). 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: A-9758 | A9758 | A 9758

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