A-9758
Modify Date: 2025-08-26 11:21:30
A-9758 structure
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Common Name | A-9758 | ||
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| CAS Number | 2055271-22-0 | Molecular Weight | 527.36 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C25H23Cl2F3N2O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of A-9758A-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]. |
| Name | A-9758 |
|---|
| Description | 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]. |
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| Related Catalog | |
| Target |
IC50: 5 nM (RORγt), 73 nM (RORα), 1370 nM (RORβ)[1] |
| 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]. |
| References |
| Molecular Formula | C25H23Cl2F3N2O3 |
|---|---|
| Molecular Weight | 527.36 |
| InChIKey | NVDKGFYFKVWJLJ-UHFFFAOYSA-N |
| SMILES | Cc1cc(C(F)(F)F)cc2c1cc(Cc1c(Cl)ccc(C(=O)N3CCC(C(=O)O)CC3)c1Cl)n2C |