A-9758 

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].

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.

527.36

C₂₅H₂₃Cl₂F₃N₂O₃

2055271-22-0

Room temperature in continental US; may vary elsewhere.

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

• [1]. Gauld S, et al. Inhibition of IL-23 mediated inflammation with a novel small molecule inverse agonist of RORgt. J Pharmacol Exp Ther. 2019 Aug 2. pii: jpet.119.258046.  [Content Brief]