2055271-22-0
2055271-22-0 structure
- Name: A-9758
- Chemical Name: A-9758
- CAS Number: 2055271-22-0
- Molecular Formula: C25H23Cl2F3N2O3
- Molecular Weight: 527.36
- Catalog: Signaling Pathways Immunology/Inflammation Interleukin Related
- Create Date: 2019-09-09 17:10:50
- Modify Date: 2024-01-07 09:01:09
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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].
| 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 |