TLR7 Agonist

PF-4878691 (3M-852A) is an orally active TLR7 agonist. PF-4878691 has the innate immune response activity, antiviral efficacy against HCV, and can be used for the research of cancer.

Resiquimod-d₅ is deuterium labeled Resiquimod. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α.

TLR7/8 agonist 4 (compound 41) is a potent TLR7/8 agonist. TLR7/8 agonist 4 has anti-cancer activity.

AXC-715 (T785) trihydrochloride is a TLR7/TLR8 dual agonist. AXC-715 trihydrochloride 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.

LHC-165 is a TLR7 agonist. LHC-165 has potential to used in study of solid tumors.

AXC-715 (T785) hydrochloride is a TLR7/TLR8 dual agonist. AXC-715 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.

Bropirimine (U-54461; U-54461S; PNU-54461) is an orally active TLR7 agonist. Bropirimine inhibits RANKL-induced osteoclast differentiation of mouse bone marrow-derived macrophages (BMMs). Bropirimine exhibits dose-dependent direct inhibitory effects on colony formation of cultured KK-47 and 724 cells. Bropirimine can be used for the study of cancers and bone metabolic disorders such as osteoporosis.

SM-324405 is a TLR7 agonistic antedrug (EC₅₀ = 50 nM), with pEC₅₀ values of 7.3 and 6.6 for human TLR7 and Rat TLR7, respectively. SM-324405 is used for immunoresearch of allergic diseases. An antedrug is defined as a locally active compound that is designed to be rapidly metabolized to an inactive form upon entry into the circulation and prevents systemic toxicity by losing its agonistic activity in a plasmatic environment.

TLR7/8 agonist 6 is a TLR7/8 agonist with EC₅₀s of 0.18 μM and 5.34 μM in TLR7 or TLR8 HEK-SEAP reporter cells, respectively. TLR7/8 agonist 6 potently stimulates production of TNFα, IFNγ, and IL-1β. TLR7/8 agonist 6 can be used for research on cancer and infectious diseases.

MTvkPABC-P5d TFA, a TLR7 agonist, is an immune stimulant. MTvkPABC-P5d TFA can be used for synthesis of immune-stimulating antibody conjugates (ISACs).

GSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC₅₀s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 is used for asthma.

L07-2 is a TLR7/8 agonist. L07-2 is a linker-toxin building block that can be used to synthesize immunostimulatory antibody conjugates (ISACs) for cancer research. L07-2 can be used to studies related to tumors such as non-small cell lung cancer.

SMU-L11 is a specific TLR7 agonist (EC₅₀=0.024 μM), which recruits MyD88 adapter protein and activates downstream NF-κB and MAPK signaling pathways. In murine models, SMU-L11 significantly enhances immune cell activation and promotes the proliferation of CD4⁺ T and CD8⁺ T cells, thereby directly killing tumor cells and inhibiting tumor growth. SMU-L11 can be used for cancer research, and also has the potential for studying immune system diseases.

TLR7 agonist 20 hydrochloride is a selective Toll-like receptor 7 (TLR7) agonist with an EC₅₀ of 0.22 μM. TLR7 agonist 20 hydrochloride, as an immunostimulant and vaccine adjuvant, enhances the production of anti-spike protein antibodies, increases IgG2b and IgG2c levels, and thereby drives Th1-type immune responses in mice. TLR7 agonist 20 hydrochloride can be used in studies related to non-inflammatory potent vaccine adjuvants.

MC-Val-Cit-PAB-Amide-TLR7 agonist 4 formic (example 15) is a HER2-TLR7 and HER2-TLR8 immune agonist conjugate.

TLR7 agonist 4 is a TLR7 agonist with pro-inflammatory cytokine-stimulating activity. TLR7 agonist 4 modulates TLR7 activity to stimulate the production of pro-inflammatory cytokines. TLR7 agonist 4 stimulates mouse bone marrow-derived macrophages to produce the pro-inflammatory cytokine TNFα. TLR7 agonist 4 can be conjugated with antibodies to form conjugates. TLR7 agonist 4 is applicable to cancer research.

MC-Val-Cit-PAB-Amide-TLR7 agonist 4 (example 15) is a HER2-TLR7 and HER2-TLR8 immune agonist conjugate.

TLR7 agonist 6 (compound IIb-19) is an TLR7 agonist with an EC₅₀ value of 1.0 nM.

TLR7/8 agonist 8 (compound 24m) is a potent toll-like receptor 7/8 (TLR7/8) dual agonist, with EC₅₀s of 27 and 12 nM for hTLR7 and hTLR8, respectively. TLR7/8 agonist 8 can improve the antitumor activity of PD-1/PD-L1 blockade.

Sotirimod (R850) is a TLR7 agonist and immunomodulator. Sotirimod inhibits Apoptosis. Sotirimod is applicable to research related to actinic keratosis, early cervical HPV infection, and precancerous lesions of colorectal cancer.