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Chemical Structure : TAK-828F
Catalog No.: PC-63177Not For Human Use, Lab Use Only.
TAK-828F (TAK-828) is a potent, selective, orally available RORγt inverse agonist with binding IC50 of 1.9 nM and reporter IC50 of 6.0 nM, displays excellent selectivity (>5,000-fold) against other ROR isoforms and nuclear receptors.
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TAK-828F (TAK-828) is a potent, selective, orally available RORγt inverse agonist with binding IC50 of 1.9 nM and reporter IC50 of 6.0 nM, displays excellent selectivity (>5,000-fold) against other ROR isoforms and nuclear receptors.
TAK-828F shows robust and dose-dependent inhibition of IL-17A expression after oral administration at 0.3, 1 and 3 mg/kg bid in the mouse IL-23-induced cytokine expression model.
TAK-828F also demonstrates dose-dependent inhibition of RORγt regulated gene expression such as IL-17F, IL-22, and IL23 receptor, but no effect against IFN-γ expression.
TAK-828F significantly reduces the development of clinical symptoms in mouse experimental autoimmune encephalomyelitis model.
| M.Wt | 509.578 | |
| Formula | C28H32FN3O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Kono M, et al. J Med Chem. 2018 Mar 14. doi: 10.1021/acs.jmedchem.8b00061.
2. Shibata A, et al. Biochem Pharmacol. 2018 Jan 30;150:35-45.
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