A-9758 is aRORγligand and a potent, selectiveRORγtinverse agonist (IC₅₀=5 nM), and exhibits robust potency againstIL-17Arelease. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuatesIL-23driven 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 IC₅₀of 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].

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.