| Description | RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist(human RORγt-LBD with an IC50 of 19 nM). |
| In vitro | RORγt Inverse agonist 8 is a potent inhibitor of RORγt and binds to the ligand binding domain (LBD) of RORγt. RORγt Inverse agonist 8 results in complete attenuation of IL-17A secretion in a concentration-dependent manner (IC50 of 60 nM in HUT78 cells). RORγt Inverse agonist 8 selectively suppresses human Th17 and Tc17 cell differentiation. RORγt Inverse agonist 8 reduces Th17 cell-associated mRNA expression including IL17A, IL17F, IL26, IL23R and CCR6 in a concentration-dependent fashion. |
| In vivo | antigen-induced arthritis (AiA) responses in Lewis rats ameliorated by RORγt Inverse agonist 8. |
| Target activity | RORγt:19 nM |
| molecular weight | 475.59 |
| Molecular formula | C26H33N7O2 |
| CAS | 2079892-79-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Guendisch U, et al. Pharmacological inhibition of RORγt suppresses the Th17 pathway and alleviates arthritis in vivo. PLoS One. 2017 Nov 20;12(11):e0188391. |