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Chemical Structure : A-9758
Catalog No.: PC-73062Not For Human Use, Lab Use Only.
A-9758 (A9758) is a selective, small molecule inverse agonist of retinoid-related orphan receptor gamma t (hRORγt IC50=38 nM).
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A-9758 (A9758) is a selective, small molecule inverse agonist of retinoid-related orphan receptor gamma t (hRORγt IC50=38 nM).
A-9758 also inhibits mouse RORγ transactivation with similar activity (20 nM) and is equally active on dog and rat RORγ (25 and 64 nM, repectively).
A-9758 inhibits TCR-mediated IL-17A secretion with an IC50 of 100 and 38 nM in human CD4+ T cells and in vitro differentiated mouse Th17 cells, respectively.
A-9758 exhibits robust potency against IL-17A release both in vitro and in vivo, significantly attenuates IL-23 driven psoriasiform dermatitis.
A-9758 exhibits efficacy in an ex vivo human whole blood assay, is efficacious in human IL-17 related diseases.
| M.Wt | 527.365 | |
| Formula | C25H23Cl2F3N2O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Gauld S, et al. J Pharmacol Exp Ther. 2019 Oct;371(1):208-218.
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