tlr 8

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

TLR7/8-IN-1, a crystalline TLR7/TLR8 inhibitor from patent WO2019220390 (compound 2b), is a valuable compound for autoimmune disease research.

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

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 2 hydrochloride is a highly potent and selective agonist for human TLR8, with an EC50 of 3 nM, but demonstrates significantly weaker activity towards human TLR7 (EC50 of 33.33 μM).

TLR8 antagonist 1 (Compound 10) is a selective antagonist that can inhibit TLR8 mediated inflammation and signaling pathways. TLR8 antagonist 1 reduces MyD88 recruitment and inhibits NF - κ B and IRF pathways, exhibiting certain anti-inflammatory activity.

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.

TLR7/8 agonist 1 is a toll-like receptor TLR7/TLR8 agonist with anticancer and antiviral activities and can be used to study immune-related diseases.

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.

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 agonist9 (Compound II-77) functions as an agonist for Toll-like receptor 8 (TLR8) with an EC50 of 0.25-1 μM. This compound is stable in human and mouse plasma and effectively induces the secretion of the cytokine TNFα with an EC50 of less than 1 μM. In the MC38-HER2 xenograft mouse model, TLR8 agonist9 demonstrates significant antitumor activity, achieving a tumor growth inhibition (TGI) rate of 97%.

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.

Selgantolimod is an effective and selective toll-like receptor 8 agonists for the treatment of the hepatitis B virus and human immunodeficiency virus infection.

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.

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.

Imiquimod (R 837) is an immune response modifier and a toll-like receptor 7 (TLR7) agonist with antiviral and antitumor effects. It is used in the study of external genital warts, perianal warts, cancer, and COVID-19, and is commonly employed to induce psoriasis models.

Resiquimod (R848) is an agonist of Toll-like receptors 7 and 8 (TLR7/TLR8) that induces the upregulation of cytokines including TNF-α, IL-6, and IFN-α. It possesses immunomodulatory, antitumor, and antiviral activities, and can be used to induce models of myocarditis and systemic lupus erythematosus (SLE).

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.

Telratolimod (MEDI9197) is a toll-like receptors 7/8 agonist. It has an antitumor activity.

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

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

3M-011, a potent dual toll-like receptor TLR7/8 agonist and cytokine inducer, serves as a powerful adjuvant to radiotherapy, eliciting significant local and systemic immune responses. Additionally, it effectively inhibits H3N2 influenza viral replication in the nasal cavity and exhibits strong antitumor activity[1][2][3].

Gardiquimod is a TLR7/8 agonist. When used at concentrations below 10 μM, Gardiquimod specifically activates TLR7. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells.

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