tlr8

Compound A, a potent TLR8 agonist, exhibits an EC50 of 0.052 µM and promotes the production of IL-12p40 in human PBMCs with an EC50 of 0.031 µM. This compound is applicable for research in virus resistance, infection resistance, autoimmunity, and tumor studies [1].

TLR8 Agonist 5, exhibiting potent efficacy as a TLR8 agonist, demonstrates an EC50 of 20 nM in HEK-Blue hTLR8, effectively activating the immune response.

TLR8 agonist 2 hydrochloride is a highly potent and selective agonist for human TLR8, exhibiting an EC50 of 3 nM. However, its activity towards human TLR7 is considerably weaker, with an EC50 of 33.33 μM.

TLR8 agonist 2 is a highly effective and specific compound that activates TLR8, possessing an EC 50 of 3 nM in human TLR8. Notably, TLR8 agonist 2 demonstrates lower activity towards human TLR7, with an EC 50 of 33.33 μM.

TLR8 agonist 4 was effective in inhibiting both wild-type and drug-resistant (lamivudine and entecavir) HBV strains with their IC50 values of 0.15 and 0.10 μM, respectively.

CU-CPT9b (TLR8-specific antagonist 1) is an antagonist of toll-like receptor 8 (TLR8; Kd = 21 nM). It inhibits activation of NF- B induced by the TLR8 agonist R-848 in TLR8-overexpressing HEK-Blue cells with an IC50 value of 0.7 nM.

CU-CPT-8m (TLR8-specific antagonist) is an toll-like receptor 8 (TLR8) antagonist (IC50 : 67 nM)

TLR7/8-IN-1, a crystalline TLR7/TLR8 inhibitor, is a valuable compound for autoimmune disease research[1].

CU-CPD107 is a selective agonist of toll-like receptor 8 (TLR8) and also shows activation activity against ssRNA ligands. CU-CPD107 acts as an inhibitor of TLR8 signaling in the presence of R848 (IC50=13.7 μM). CU-CPD107 exhibited coagonist activity in the presence of ssRNA, while CU-CPD107 alone could not affect TLR8 signal transduction.

Enpatoran is an inhibitor of TLR7(IC50 = 11.1 nM) and TLR8(IC50 = 24.1 nM). Enpatoran was found to be inactive against TLR3, TLR4, and TLR9 in vitro and in vivo.

CU-115 is a selective and potent TLR8 antagonist with IC50 of 1.04 µM and =>50 µM for TLR8 and TLR7, respectively. CU-115 decreases production of TNF-α and IL-1β activated by R-848 in THP-1 cells.

CU-CPT-9a is a potent TLR8 inhibitor (IC50 : 0.5 nM), that suppresses TLR8-mediated proinflammatory signaling in various cell lines and human primary cells-

Motolimod (VTX-378) (VTX-2337) is an effective and specific Toll-like receptor (TLR) 8 agonist (EC50: 100 nM), > 50-fold selectivity over TLR7.

AXC-715 hydrochloride is a TLR7/TLR8 dual agonist, can be used for synthesis of antibody-adjuvant immunoconjugates, comprising an antibody construct that binds programmed death-ligand 1 (PD-L1) linked to one or more adjuvants.

BMS-905 is a potent dual inhibitors of TLR7 and TLR8 with good selectivity against TLR9 and other family members. BMS-905 can be used in studies about the treatment of diseases such as psoriasis, arthritis, and lupus.

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

TLR7/8 agonist 8 (compound 24m) is a potent dual agonist for toll-like receptors 7 and 8 (TLR7/8), exhibiting half-maximal effective concentrations (EC50s) of 27 nM for human TLR7 (hTLR7) and 12 nM for human TLR8 (hTLR8). This compound has been shown to enhance the efficacy of PD-1/PD-L1 inhibitors in antitumor activity [1].

TL8-506 can be used in autoimmune diseases and tuberculosis research which is a specific agonist of TLR8 (EC 50 = 30 nM) [1].

CL097 is an effective agonist of TLR7 and TLR8. CL097 induces pro-inflammatory cytokines in macrophages and NADPH oxidase priming, thereby increasing the fMLF-stimulated ROS production.

AXC-715 trihydrochloride (T785 trihydrochloride) is a TLR7/TLR8 dual agonist for the synthesis of antibody-adjuvanted immunocouplings. The couplings are mostly programmed death ligand 1 (PD-L1) attached to one or more antibody structures of the adjuvant.

Enpatoran (M5049) hydrochloride is a potent and orally active dual inhibitor of TLR7/8 with IC50 values of 11.1 nM and 24.1 nM in HEK293 cells, respectively. This compound specifically inhibits TLR7 and TLR8, while showing no activity against TLR3, TLR4, and TLR9. Enpatoran hydrochloride has the ability to block both synthetic molecule ligands and natural endogenous RNA ligands. Additionally, it demonstrates excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be a valuable tool for studying and modulating both innate and adaptive autoimmunity. [1]

TLR7/8 agonist 6 (Compound 4), an imidazoquinoline derivative, is a potent TLR7/8 agonist with IC50 values of 0.18 and 5.34 μM for TLR7 and TLR8, respectively. TLR7/8 Antagonist

CU-CPT17e is a potent agonist of TLR(TLR3, TLR8, and TLR9).

TLR7/8 antagonist 2 (Compound 15) is a highly potent and orally active agonist of TLR7/8, exhibiting IC50 values of 4.9 and 0.6 nM for TLR7 and TLR8, respectively. Its strong affinity for these receptors makes it a promising candidate for the treatment and investigation of autoimmune diseases, including lupus erythematosus, which is associated with inappropriate activation of TLR7 and TLR8. Consequently, TLR7/8 antagonist 2 represents a valuable tool for research in the field of autoimmune diseases [1].

MC-Val-Cit-PAB-Amide-TLR7 agonist 4 (example 15) is a conjugate that acts as an immune agonist targeting both HER2-TLR7 and HER2-TLR8 pathways [1].

CL075 (3M002) is a selective TLR8 agonist.CL075 has immunomodulatory activity by triggering the MyD88-dependent signaling pathway, activating NF-κB and IRF7 to elicit the production of inflammatory cytokines and type I interferon (IFN).

TLR7/8 Antagonist 1 (Compound 16c), an imidazoquinoline derivative, is a potent TLR7/8 agonist with IC50 values of 3.91 and 2.19 μM for TLR7 and TLR8, respectively. rel-O-2050 (TLR-2050) is a key target for drug development in infectious diseases, cancer and autoimmune diseases.

TLR7/8 agonist 1 dihydrochloride (TLR7/8 agonist-5d) is a TLR7/8 agonist which shows prominent immunostimulatory activities.

CL097 hydrochloride is a potent TLR7 and TLR8 agonist. CL097 hydrochloride induces pro-inflammatory cytokines in macrophages and NADPH oxidase priming, thereby increasing the fMLF-stimulated ROS production [2].

TLR7/8 agonist 3 is a potent agonist of TLR7 and TLR8.