TLR7/8 Ligands

TLR7-TLR8 pathway

InvivoGen provides a growing library of synthetic ligands known to bind TLR7 and/or TLR8

Toll-like receptor (TLR) 7 and TLR8 are endosomal receptors that play an important role in the immune response to viral infection. Depending on the binding site of the receptor, they recognize GU-rich short single-stranded RNA (ssRNA) as their natural ligand, as well as small synthetic molecules, such as imidazoquinolines and nucleoside analogs.

Several preclinical studies and clinical trials suggest that these synthetic TLR7/8 ligands have the potential to be powerful immunomodulators, vaccine adjuvants, and cancer therapeutics. However, challenges in achieving suitable efficacy while avoiding toxicities remain a significant barrier.  Defining their synergistic role in combination with established as well as emerging treatments will enhance their significant potential to further improve therapeutic outcomes. 

InvivoGen provides the most comprehensive choice of TLR7, TLR7/8, and TLR8 agonists and antagonists. Our growing library includes:

• Single-stranded RNAs - RNA homopolymer ssPolyU and GU-rich oligonucleotides, such as ssRNA40, derived from HIV-1.
   
• Base Analogs - imidazoquinoline compounds, such as Resiquimod (R848) and R837, the thiazoquinoline compound CL075, and nucleoside analogs, such as Loxoribine.
   
• Antagonists - the specific inhibitor of TLR8 CU-CPT9a, as well as the dual and selective inhibitor for TLR7 and TLR8 M5049.

The specificity, activity, and potency of each ligand are vigorously tested using our HEK-Blue™ and HEK-Dual™ TLR reporter cell line collection. Moreover, each lot is highly pure and functionally tested.  For vaccination studies, InvivoGen supplies various TLR7/8 ligands (e.g. R848, R837)  in a pre-clinical VacciGrade™.  

VacciGrade™ is a high-quality pre-clinical grade. VacciGrade™ products are filter-sterilized (0.2 µm) and filled under strict aseptic conditions in a clean room*. The absence of bacterial contamination is assessed by a sterility test using a pharmacopeia-derived assay. The level of bacterial contaminants (endotoxins and lipoproteins) in each lot is verified using a LAL assay and/or a TLR2 and TLR4 reporter assay.

Read our review about TLR7 and TLR8.