| Description | TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (IC50=1.9 nM, reporter gene IC50=6.1 nM). |
| In vivo | In mice with IL-23-induced cytokine expression model, TAK-828F (0.3, 1, and 3 mg/kg; orally administered; b.i.d.; 28 days; ) shows robust and dose-dependent inhibition of IL-17A expression with an ED80 of 0.5 mg/kg. |
| Target activity | RORγt, binding IC50:1.9 nM , RORγt, reporter gene IC50:6.1 nM |
| molecular weight | 509.57 |
| Molecular formula | C28H32FN3O5 |
| CAS | 1854901-94-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Kono M, et al. Discovery of [ cis-3-({(5 R)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1 H-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5 H)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist. J Med Chem. 2018 Apr 12;61(7):2973-2988. |