TLR7 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 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 agonist26 (Compound 4) serves as an effective Toll-like receptor7 (TLR7) agonist with an EC50 value of 225.5 nM. It exhibits immunopotentiating effects.

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 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 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.

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].

TLR7 agonist 30 (compound 2) is a drug-linker conjugate used in ADCs. It comprises TLR7 agonist (compound 1) and a cleavable linker, exhibiting potent anti-tumor activity.

Imiquimod hydrochloride (R 837 hydrochloride), a selective toll-like receptor 7 (TLR7) agonist, functions as an immune response modifier with in vivo antiviral and antitumor properties, and is utilized in researching external genital and perianal warts, cancer, and COVID-19 [1] [2].

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).

Gardiquimod diTFA, an imidazoquinoline analog and TLR7 8 agonist, inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs), and specifically activates TLR7 at concentrations below 10 μM. As an immune system modifier and reverse transcriptase inhibitor, it serves as a novel therapeutic agent to block systemic and mucosal transmission of HIV-1.[1][2]

CL097 hydrochloride is a potent TLR7 and TLR8 agonist. CL097 hydrochloride induces pro-inflammatory cytokines in macrophages and NADPH oxidase priming, thereby increasing the fMLF-stimulated ROS production [2].

UC-1V150 is a distinct TLR7 agonist, which activates cellular immune responses and exhibits anti-tumor effects. It also serves as a precursor for the synthesis of ISAC molecules, known as immune-stimulating antibody conjugates [1] [2].

Ruzotolimod, an agonist of TLR7, exhibits promising potential for investigating HBV, COVID-19, and SARS-CoV-2 infections (WO2021130195A1)[1].

TLR7 8 antagonist 2 (Compound 15) is a highly potent and orally active agonist of TLR7 8 with IC50 values of 4.9 nM for TLR7 and 0.6 nM for TLR8, making it a promising candidate for treating and investigating autoimmune diseases like lupus erythematosus, which involves inappropriate activation of TLR7 and TLR8. Consequently, TLR7 8 antagonist 2 is a valuable tool for autoimmune disease research [1].

TLR7 agonist 12 (example 20), a purine nucleoside analog, functions as a TLR7 agonist with broad antitumor activity, particularly against indolent lymphoid malignancies. Its anticancer mechanisms include DNA synthesis inhibition, apoptosis induction, among others [1] [2].

NCI 126224, a toll-like receptor 4 (TLR4) antagonist, demonstrates selective inhibition of nitric oxide (NO) production in RAW 264.7 macrophages, triggered by the TLR4 agonist LPS (IC50 = 0.31 µM), as opposed to minimal effects on NO production induced by agonists for TLR7/8 (R-848), TLR1/2 (Pam3CSK4), and TLR3 (poly(I:C)). Nevertheless, it also effectively inhibits NO production initiated by the TLR2/6 agonist FSL-1 at an IC50 of 0.6 µM in the same cell line. Moreover, NCI 126224 suppresses LPS-induced NF-κB activity in BV-2 microglial cells and reduces LPS-triggered increases in IL-1β and TNF-α levels in RAW 264.7 macrophages with IC50 values of 5.92, 0.42, and 1.54 µM, respectively.