tlr-7 agonist 2

TLR7 agonist 2 (TLR7-IN-1) is a specific and effective Toll-like Receptor 7 (TLR7) agonist (LEC=0.4 μM).

TLR7 agonist27 (compound 24) is an effective TLR7 agonist with an EC50 of 238.1 nM. It exhibits weak agonistic activity towards NOD2 (nucleotide-binding oligomerization domain 2) with an EC50 of 6.2 μM. TLR7 agonist27 serves as a potent immunostimulant and can be utilized as a vaccine adjuvant and/or an immunotherapeutic agent.

TLR7 agonist28 (compound 3) is a potent TLR7 agonist. This compound can be combined with anti-tumor monoclonal antibodies (mAb) for use in cancer immunotherapy.

TLR7 agonist 29 (Compound 1) is an activator of TLR7, displaying an EC50 of 5.2 nM for human TLR7 and 48.2 nM for mouse TLR7. It can activate bone marrow-derived macrophages (BMDM) and stimulate myeloid cells within the tumor microenvironment, enhancing the expression of PD-L1, CD86, and IFN-α. Additionally, TLR7 agonist 29 can serve as a payload for synthesizing ADCs.

TLR7 agonist22 (Compound 11a) is a selective TLR7 agonist with an IC50 value of 25.86 μM. It inhibits the secretion of cell HBsAg and effectively activates TLR7, inducing the release of TLR7-regulated cytokines IL-12, TNF-α, and IFN-α in human PBMC cells. TLR7 agonist22 shows promise for developing novel immunomodulatory drugs in HBV research.

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.

TLR7 agonist20 (compound 23) is an imidazoquinoline analogue. It acts as a potent and specific TLR7 agonist with an EC50 value of 0.23 μM for hTLR7. This compound exhibits strong adjuvant activity on spike antibody levels and induces a robust T helper cell 1 (Th1) response, increasing IgG2b and IgG2c alongside IgG1.

TLR7 agonist23 (compound 12b) is a potent agonist of Toll-like receptor-7 (TLR7), with an EC50 value of 0.15 uM. It is suitable for research in immune diseases.

TLR7 agonist24 (Compound 21) is an agonist of TLR7 with an EC50 of 3.72 μM. When combined with Aluminum Hydroxide, it can be employed as a vaccine adjuvant to enhance the immune response to antigens from SARS-CoV-2 and hepatitis B.

TLR7 agonist20 hydrochloride is an imidazoquinoline analog that functions as a potent and specific agonist for TLR7, with an EC50 value of 0.23 μM against hTLR7. It demonstrates strong adjuvant activity in enhancing spike antibody levels and induces a robust T helper cell 1 (Th1) response. Additionally, it increases levels of IgG2b and IgG2c, aside from IgG1.