TAK-828F

• Description:

  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].

• UNSPSC:

  12352005

• Target:

  ROR

• Type:

  Reference compound

• Related Pathways:

  Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

• Applications:

  COVID-19-immunoregulation

• Field of Research:

  Inflammation/Immunology

• Assay Protocol:

  https://www.medchemexpress.com/TAK-828F.html

• Solubility:

  10 mM in DMSO

• Smiles:

  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

• Molecular Formula:

  C28H32FN3O5

• Molecular Weight:

  509.57

• References & Citations:

  [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.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• CAS Number:

  [1854901-94-2]