TAK-828F 

TAK-828F is a potent, selective, and orally available retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist (binding IC₅₀=1.9 nM, reporter gene IC₅₀=6.1 nM). TAK-828F shows excellent RORγt isoforms selectivity (>5000-fold selectivity against human RORα and RORβ)^[1].

IC50: 1.9 nM (RORγt, binding IC₅₀), 6.1 nM (RORγt, reporter gene IC₅₀)^[1]

TAK-828F (0.3, 1, and 3 mg/kg; orally administered; b.i.d.; 28 days; in mice with IL-23-induced cytokine expression model) shows robust and dose-dependent inhibition of IL-17A expression with an ED₈₀ of 0.5 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

509.57

C₂₈H₃₂FN₃O₅

1854901-94-2

CC1(C)C2=C(F)C=C(NC([C@@H]3N(C([C@@H]4C[C@H](CC(O)=O)C4)=O)CCC5=C3C=CC(OC)=N5)=O)C=C2CC1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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 Reti  [Content Brief]