TLR7 Agonist

TLR7/8 agonist 11 (compound 30) is a potent agonist of hTLR7 and hTLR8, with EC₅₀s of 31.1 nM and 13.1 nM, respectively. TLR7/8 agonist 11 plays an important role in adaptive and innate immune responses.

AYK004 is a TLR7/8 agonist that enhances immune responses by activating the TLR signaling pathway. AYK004 is an adenine derivative with a favorable hydrophilic-lipophilic balance, which improves the loading capacity and stability in immunoadjuvant systems such as liposomes, while reducing the side effects of the immunoadjuvant system in systemic immunity .

FGT-4 is a FR-β-targeted chimeric molecule. FGT-4 acts as a TLR7 agonist. FGT-4 binds to FR-β to enable delivery to tumor-associated macrophages and myeloid-derived suppressor cells. FGT-4 promotes the secretion of iNOS (associated with M1 macrophages) and the pro-inflammatory cytokine IL-6, and enhances the proliferation of cytotoxic CD8+ T cells. FGT-4 can be used for the research of breast cancer.

3M-011 is a potent dual toll-like receptor TLR7/8 agonist and a cytokine inducer. 3M-011 significantly inhibits H3N2 influenza viral replication in the nasal cavity. 3M-011 is also a potent adjuvant to radiotherapy that induces local and profound systemic immune responses during radiotherapy. 3M-011 strongly has antitumor action.

MTT5 is a toll-like receptor 7 (TLR7) agonist. MTT5 can couple with Deruxtecan (HY-13631E) and exert anti-tumor activity in HER2 positive solid tumors through tumor cell killing and immune activation.

SMU-L11-R is a selective TLR7 agonist with an EC₅₀ of 0.012 μM for human TLR7. SMU-L11-R specifically activates TLR7, recruits  MyD88, and triggers MAPK/NF-κB pathways, leading to TNF-α/IL-1β/IL-6 secretion in both mouse and human peripheral blood mononuclear cells. SMU-L11-R promotes M1-like macrophage polarization. SMU-L11-R exhibits excellent synergistic anti-tumor effects with PD-L1 inhibitors by upregulating CD8⁺T cells. SMU-L11-R shows potential in colorectal cancer studies.

TLR7 agonist 8 is a TLR7 agonist with an EC₅₀ of 0.12 nM for TLR7 and an EC₅₀ of 0.76 nM for IL-6 induction. TLR7 agonist 8 can be used for research on diseases such as fibrosis, inflammatory diseases, cancer, or pathogen infections.

TLR7 agonist 26 (Compound 4) is a potent Toll-like receptor 7 (TLR7) agonist, with an EC₅₀ of 225.5 nM. TLR7 agonist 26 shows immunopotentiating effects.

AZ12441970 is a potent and selectiveToll-like receptor 7 (TLR7) agonist, exhibiting pEC₅₀s of 6.8 and 6.6 for human and rat TLR7. AZ12441970 shows efficacy in a mouse allergic airway model with minimal induction of systemic IFN-α. AZ12441970 can be used for allergic airway disease research.

TLR7 agonist 14 (compound 17b) is a highly potent TLR7 agonist with an EC₅₀ of 18 nM. TLR7 agonist 14 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations.

UM-3006 is a highly efficient TLR7/8 agonist that enhances immune responses by activating the TLR signaling pathway. UM-3006 holds significant research and application potential in the fields of vaccine adjuvants and immune diseases.

Isatoribine is a TLR7 agonist. Isatoribine is used in the study of chronic hepatitis C virus (HCV) infection.

BBIQ (GMP) is BBIQ (HY-111582) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BBIQ is a potent and selectively toll-like receptor 7 (TLR7) agonist with an EC₅₀ of  59.1 nM. BBIQ is a powerful vaccine adjuvant that enhances innate immune responses.

Poly (U) (Polyuridylic acid) is an RNA chain that exists in a disordered extended state at room temperature and serves as a TLR7 ligand. Poly (U) produces distinguishable blocking effects when transported through α-hemolysin nanopores. Poly (U) forms a triple helix with adenosine or adenosine monophosphate, thereby significantly promoting the nucleotide bond condensation reaction between adenosine monophosphate and adenosine, while exerting minimal effects on other nucleosides. When conjugated with cationic lipids, Poly (U) specifically stimulates plasmacytoid dendritic cells to produce type I interferons.

TLR7/8 agonist 13 is an orally active dual agonist of TLR7 (lowest effective concentrations (LEC) [hTLR7] = 1.6 μM) and TLR8 (LEC [hTLR8] = 1.6 μM). TLR7/8 agonist 13 exhibits agonistic activity against human peripheral blood mononuclear cells (hPBMCs) (LEC [hPBMC] = 0.5 μM). TLR7/8 agonist 13 induces endogenous IFNα, activating myeloid dendritic cells and monocytes toward a TH1 phenotype in mice and cynomolgus monkeys. TLR7/8 agonist 13 reduces viral load and HBV surface antigen expression in a mouse model of chronic AAV-HBV infection. TLR7/8 agonist 13 has the potential to indirectly induce IFNγ, which may promote HBV antigen-specific CD8 T cell-mediated responses. TLR7/8 agonist 13 can be used to study hepatitis B virus.