TLR7/8 agonist 1 is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.

TLR7/8 agonist 1 (Compound 5d) shows prominent immunostimulatory activities. TLR7/8 agonist 1 serves as a convenient precursor for the covalent attachment of fluorophores without significant loss of activity.TLR7/8 agonist 1 retains TLR7-agonistic activity with an EC₅₀ of 20 nM. TLR7/8 agonist 1 is covalently coupled directly to commercially-available fluorescein isothiocyanate and rhodamine B isothiocyanate. TLR7/8 agonist 1 (Compound 1) shows substantially different agonistic potencies in human TLR7 (50 nM) and TLR8 (55 nM) primary screens.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . Shukla NM, et al. Syntheses of fluorescent imidazoquinoline conjugates as probes of Toll-like receptor 7. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6384-6.  [Content Brief]

  . Beesu M, et al. Structure-Based Design of Human TLR8-Specific Agonists with Augmented Potency and Adjuvanticity. J Med Chem. 2015 Oct 8;58(19):7833-49.  [Content Brief]