tlr7/tlr8

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.

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).

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.

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.

MC-Val-Cit-PAB-Amide-TLR7 agonist 4 TFA is the trifluoroacetate form of MC-Val-Cit-PAB-Amide-TLR7 agonist 4. MC-Val-Cit-PAB-Amide-TLR7 agonist 4 is a HER2-TLR7 and HER2- TLR8 immune agonist complexes with potential antitumor activity by activating the TLR7 and TLR8 signaling pathways and enhancing immune responses.

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.

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

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.

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

TLR7/8 agonist 11 (compound 30) serves as a powerful agonist for hTLR7 and hTLR8, exhibiting EC50 values of 31.1 nM and 13.1 nM, respectively. This compound is crucial in the functioning of both adaptive and innate immune responses.

INI-4001, a TLR7/8 agonist, exhibits EC50 values of 1.89 μM and 4.86 μM for TLR7 and TLR8, respectively. This compound induces signal transduction and SEAP production through TLR7 and TLR8. Furthermore, INI-4001 stimulates the production of high-affinity, fentanyl-specific antibodies, effectively preventing fentanyl from crossing the human blood-brain barrier. It serves as an effective adjuvant in anti-fentanyl vaccines for individuals with opioid use disorder (OUD).

TLR7 agonist21 (Compound 27B) is a selective activator of Toll-like receptor 7 (TLR7), with an EC50 of 17.53 nM for human TLR7 and 41.7 nM for mouse TLR7. It induces the secretion of pro-inflammatory cytokines, including IL-6, TNF-α, IFN-α1, and IL-4. Acting as a vaccine adjuvant, TLR7 agonist21 enhances IgG and IgA levels, offering protection for mice against influenza virus infection.

KBD4466 is a potent oral inhibitor of TLR7 and TLR8, with IC50 values of 0.9 nM and 2.8 nM, respectively. This compound effectively suppresses the inflammatory cytokines IL-6 and IFN-α. KBD4466 has shown to improve disease progression and increase survival rates in the BXSB/MpJ mouse model of systemic lupus erythematosus (SLE). It is suitable for research into autoimmune diseases.

TLR7/8 agonist 13 is an orally active dual agonist of TLR7 (with a lowest effective concentration (LEC) [hTLR7] of 1.6 μM) and TLR8 (LEC [hTLR8] of 1.6 μM). It acts on human peripheral blood mononuclear cells (hPBMC) with agonistic activity (LEC [hPBMC] = 0.5 μM). In mice and cynomolgus monkeys, TLR7/8 agonist 13 induces endogenous IFNα, activates myeloid dendritic cells and monocytes, promoting their differentiation towards a TH1 phenotype. In chronic AAV-HBV mouse models, it reduces viral load and HBV surface antigen levels. TLR7/8 agonist 13 has the potential to indirectly induce IFNγ, facilitating the response of HBV antigen-specific CD8 T cells. This compound is useful for hepatitis B virus research.

SMU-R39 is a TLR7 and TLR8 antagonist with IC50 values of 3.22 μM and 0.24 μM, respectively. It binds to recombinant mTLR7 protein (KD= 2.36 μM) and recombinant hTLR8 protein (KD= 105 nM). SMU-R39 inhibits downstream NF-κB and MAPK signaling pathways, reducing the secretion and transcription of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in PBMCs and THP-1 cells. In an Imiquimod (IMQ)-induced psoriasis mouse model, SMU-R39 exhibits anti-inflammatory activity and may be used for researching autoimmune diseases such as psoriasis.

TLR7/8 agonist 14 is a dual-target agonist of TLR7 and TLR8, with EC50 values of 75 μM for TLR7 and 96 μM for TLR8. This compound enhances the secretion of pro-inflammatory cytokines TNF-α, IL-1β, IL-8, and IFN-γ, while also increasing cytokine secretion and CD86 expression levels. TLR7/8 agonist 14 is applicable in colorectal cancer research.

Bazlitoran is an oligonucleotide that functions as an antagonist of TLR7, TLR8, and TLR9.

Bazlitoran sodium is an oligonucleotide and acts as an antagonist of TLR7, TLR8, and TLR9.

Enpatoran hydrochloride (M5049 hydrochloride) is an orally active, selective, and potent TLR7/8 inhibitor with antiviral activity for the study of autoimmune diseases and COVID-19 pneumonia.

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

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.

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.