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.

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.

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).

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.

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.

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).

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.

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

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.