Toll-like Receptors

Toll-Like Receptor 7 Ligand II is a cell-permeable hydroxyadenine compound which acts as a potent and highly specific TLR7 (toll-like receptor 7) agonist without any detectable activity towards TLR2/3/5/8/9. It is shown to be 10-times more potent than R848 in stimulating the production of TLR7-dependent cytokines in cultures in vitro .

Isatoribine is a novel guanosine analogue showing immunostimulatory activity both in vivo and in vitro.

MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively.

IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. It inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein.

TLR7 agonist 1 is a potent, selective and oral TLR7 agonist with an IC50 of 90 nM.

LHC-165 is a TLR7 agonist. Has potential to treat solid tumors.

MMG-11 is a potent and selective human TLR2 antagonist with low cytotoxicity.

AN-3485 is a benzoxaborole analog, Toll-Like Receptor(TLR) inhibitor with IC50 values ranging from 18 to 580 nM.

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

TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis.