Toll-like Receptor (TLR) Agonist

Mosedipimod is a monoacetyldiaglyceride that can be isolated from Cervus nippon Temminck. Mosedipimod is an orally active Toll-Like Receptor signaling inhibitor. Mosedipimod attenuates airway infammation by reducing myeloperoxidase expression in lung tissue. Mosedipimod is used in chronic obstructive pulmonary disease research.

TLR8 agonist 2 hydrochloride is a potent and selective TLR8 agonist with an EC₅₀ of 3 nM for human TLR8. TLR8 agonist 2 hydrochloride shows less active against human TLR7 (EC₅₀ of 33.33 μM).

TLR8 agonist 2 is a potent and selective TLR8 agonist with an EC₅₀ of 3 nM for human TLR8. TLR8 agonist 2 shows less active against human TLR7 (EC₅₀ of 33.33 μM).

TLR7/8 agonist 7 (compound 10) is a TLR7/8 agonist. TLR7/8 agonist 7 activates a variety of immune cells and it can be used to synthesize immune stimulating antibody conjugate (ISAC) molecules. TLR7/8 agonist 7 can be used for the research of immunity.

UC-1V150 is a specific TLR7 (Toll-like receptor) agonist that stimulates cellular immune responses and has anti-tumor activity. UC-1V150 can be used to synthesize ISAC (Immune-Stimulating Antibody Conjugates) molecule.

NOD1/TLR7 agonist-1 is a dual NOD1 and TLR7 agonist. NOD1/TLR7 agonist-1 exhibits adjuvant effects in mouse vaccine models and induces increased ovalbumin-specific IgG titers. NOD1/TLR7 agonist-1 can be used for research on immune-related diseases.

FITC-labeled ODN 1668 (sodium), a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. FITC-labeled ODN 1668 (sodium) can be used to evaluate CpG ODN cellular uptake and localization by confocal laser-scanning microscopy (excitation 495 nm, emission 520 nm) or flow cytometry.

TLR7 agonist 31 (Compound 116) is a TLR7 agonist, with an EC₅₀ of 31 nM. TLR7 agonist 31 can be used in the research of cancer.

TLR7 agonist 17 (compound 20) is a potent TLR7 agonist with EC₅₀ values of 12 nM and 17 nM for hTLR7 and mTLR7, respectively. TLR7 agonist 17 shows anticancer activity.

TLR7 agonist 19 (Compound 14) is a Toll-like receptor 7 (TLR7) agonist with excellent pharmacokinetic properties and synergistic antitumor activity.

NSF-951 (ZINC67299692) is a TLR4 agonist (K_d = 16.01 μM). NSF-951 activates the p38 and JNK kinase pathways. NSF-951 induces IL-6 and TNF-α responses and upregulates CD80 and CD86 expression. In mouse immunization studies, NSF-951 alone or in combination with Alum enhances antigen-specific antibody and T cell responses.

NOD2/TLR4 agonist-1 (Compound 2) is a NOD2/TLR4 dual agonist. NOD2/TLR4 agonist-1 lacks immunostimulatory activity and serves as an important negative control in research.

Nelitolimod, a CpG oligonucleotide, is a TLR9 agonist.

GNKG168 is a synthetic, 21-mer, unmethylated CpG oligodeoxynucleotide. It acts as a TLR9 agonist with immunostimulatory activity.

WYJ-2 is a selective agonist for toll-like receptor 2/1 (TLR2/1) with EC₅₀ of 18.57 nM in human TLR2 and TLR1 transient-cotransfected HEK 293T cells. WYJ-2 induces pyroptosis and exhibits anticancer activity against non-small cell lung cancer (NSCLC).

3D-Monophosphoryl Lipid A-5 (3D-MPLA-5) triethylamine is a TLR agonist that can be used as an adjuvant for vaccines to enhance their immunogenicity.

SMU-C68 is a highly selective small-molecule TLR1/2 heterodimer agonist (EC₅₀=0.009 μM). SMU-C68 activates NF-κB and MAPK pathways to promote pro-inflammatory cytokine release (e.g., TNF-α, IL-1β). SMU-C68 is promising for research of cancers.

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

Bazlitoran (IMO-8400) is an oligonucleotide-based TLR7/8/9 antagonist. Bazlitoran blocks the activation of Toll-like receptors 7, 8, and 9. Bazlitoran inhibits cytokine responses mediated by Toll-like receptors 7, 8, and 9. Bazlitoran is associated with injection site reactions. Bazlitoran improves moderate-to-severe plaque psoriasis.

Litenimod is potent type B agonist of toll Like receptor 9 (TLR9), triggering both innate and adaptive immune response.