TLR7-agonist-1

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

TLR7 agonist 1 is a selective and oral TLR7 agonist (IC50: 90 nM).

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

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.

D18 is an immune modulator that acts as a dual agonist for TLR7 8 (with EC50 values of 24 nM for hTLR7 and 10 nM for hTLR8, respectively). It enhances the expression of PD-L1 through epigenetic regulation, thereby increasing the sensitivity of tumors to PD-1 PD-L1 blockade. Additionally, D18 functions as a cytotoxin for ADC synthesis, specifically for the ADC HE-S2 [1].

1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist known for its anti-tumor properties.

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.

GSK2245035 is a highly selective intranasal TLR7 agonist with preferential Type-1 interferon (IFN)-stimulating properties (pEC50s: 9.3 and 6.5 for IFNα and TFNα). It effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood

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.

Gardiquimod (hydrochloride) is an imidazoquinoline class TLR7 8 agonist. It can inhibit HIV-1 infection in macrophages and activated peripheral blood mononuclear cells (PBMCs). At concentrations below 10 μM, Gardiquimod (hydrochloride) specifically activates TLR7.

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 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].

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.

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]

TLR7 8 agonist 4 (compound 41) is a potent TLR7 8 agonist with demonstrated anti-cancer activity [1].

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 8 Antagonist 1 (Compound 16c), an imidazoquinoline derivative, is a potent TLR7 8 agonist with IC50 values of 3.91 and 2.19 μM for TLR7 and TLR8, respectively. rel-O-2050 (TLR-2050) is a key target for drug development in infectious diseases, cancer, and autoimmune diseases.

GSK-2245035 maleate is a selective Toll-like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties.

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].

TLR7 8 agonist 4 hydroxy-PEG6-acid hydrochloride, a Drug-Linker Conjugate for ADC synthesis, is the hydrochloride variant of TLR7 8 agonist 4 hydroxy-PEG6-acid, with the TLR7 8 agonist 4 component attached to the hydroxy-PEG6-acid linker [1].