TLR7/8 Ligands

Single-stranded RNA agonists and base analogs

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. 

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InvivoGen provides a comprehensive choice of TLR7, TLR7/8, and TLR8 agonists and antagonists. 

  • TLR7/8 Agonists - Include single-stranded RNAs, a selection of short synthetic oligonucleotides containing GU-, UG- or U-rich sequences, and base analogs, a collection of compounds featuring an heterocyclic ring and a exocyclic amino group that mimic key features of RNA bases.
     
  • TLR7/8 Antagonists - Heterocyclic compounds, containing an indole or quinoline ring, that bind TLR7/8 but block receptor activation sthe 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. 

InvivoGen also supplies VacciGrade™ TLR7/8 agonists designed for vaccination studies. 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.

More infoRead our review about TLR7 and TLR8.

TLR7/8 Ligands

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