tlr7/8

TLR7/8 agonist 3 is a potent activator of TLR7 and TLR8.

TLR7/8/9 antagonist 2 is an orally active and highly bioavailable vTLR7/8/9 antagonist. It inhibits HEK/hTLR7, HEK/hTLR8, and HEK/hTLR9 with IC50s of 0.011 μM, 0.029 μM, and 0.052 μM, respectively. TLR7/8/9 antagonist 2 can be used to study auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis.

TLR7/8 agonist 11 (compound 30) serves as a powerful agonist for hTLR7 and hTLR8, exhibiting EC50 values of 31.1 nM and 13.1 nM, respectively. This compound is crucial in the functioning of both adaptive and innate immune responses.

TLR7/8 agonist 12 (compound 9) is a human TLR7/8 agonist with EC50 values of 11 nM for hTLR7 and 150 nM for hTLR8, indicating its potential for immune modulation.

TLR7/8 agonist 12-PAB-(PEG4-Me)-Cit-Val-PEG2-amide-C2-MC (compound LIV1-IMC (12) linker-payload) serves as a linker-payload conjugate designed for the synthesis of antibody-drug conjugates (ADCs). This structure incorporates a TLR7/8 agonist (ADC payload) along with a linker.

TLR7/8 agonist 13 is an orally active dual agonist of TLR7 (with a lowest effective concentration (LEC) [hTLR7] of 1.6 μM) and TLR8 (LEC [hTLR8] of 1.6 μM). It acts on human peripheral blood mononuclear cells (hPBMC) with agonistic activity (LEC [hPBMC] = 0.5 μM). In mice and cynomolgus monkeys, TLR7/8 agonist 13 induces endogenous IFNα, activates myeloid dendritic cells and monocytes, promoting their differentiation towards a TH1 phenotype. In chronic AAV-HBV mouse models, it reduces viral load and HBV surface antigen levels. TLR7/8 agonist 13 has the potential to indirectly induce IFNγ, facilitating the response of HBV antigen-specific CD8 T cells. This compound is useful for hepatitis B virus research.

TLR7/8-IN-1, a crystalline TLR7/TLR8 inhibitor from patent WO2019220390 (compound 2b), is a valuable compound for autoimmune disease research.

TLR7/8/9-IN-1 is a potent inhibitor of Toll-like receptors 7, 8, and 9 (TLR7/8/9) with an IC50 of 43 nM.

TLR7/8 agonist 4 hydroxy-PEG10-acid [compound 9] is a drug-linker conjugate used in antibody-drug conjugates (ADC), exhibiting remarkable antitumor activity. It utilizes TLR7/8 agonist 4, a potent activator of TLR7/8, linked to hydroxy-PEG10-acid via a cleavable bond, demonstrating promising pharmaceutical potential in ADC-based therapeutics.

TLR7/8 agonist 4 TFA (compound 41) is a highly potent TLR7/8 agonist demonstrating significant anti-cancer activity.

TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride (compound 9) is a drug-linker conjugate used in antibody-drug conjugates (ADCs) with high tumor efficacy. It consists of TLR7/8 agonist 4, a potent TLR7/8 agonist, linked to the ADC linker hydroxy-PEG10-acid, which can be cleaved.

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

TLR7/8 agonist 4 (compound 41) is a potent TLR7/8 agonist with demonstrated anti-cancer activity [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 agonist 6 (Compound 4), an imidazoquinoline derivative, is a potent TLR7/8 agonist with IC50 values of 0.18 μM for TLR7 and 5.34 μM for TLR8 [TLR7/8 Antagonist].

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.

TLR7/8 agonist-7d is a useful organic compound for research related to life sciences and the catalog number is T64606.

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.

TLR7/8 agonist 7, a compound that functions as a TLR7/8 agonist, plays a pivotal role in activating various immune cells and is instrumental in the synthesis of immune-stimulating antibody conjugate (ISAC) molecules. This compound holds significant potential for research in immunology.

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].

TLR7/8 agonist 8 (compound 24m) is a potent dual agonist for toll-like receptors 7 and 8 (TLR7/8), exhibiting half-maximal effective concentrations (EC50s) of 27 nM for human TLR7 (hTLR7) and 12 nM for human TLR8 (hTLR8). This compound enhances the efficacy of PD-1/PD-L1 inhibitors in antitumor activity [1].

TLR7/8 agonist 9 (Compound 25a), with EC50 values of 40 nM for hTLR7 and 23 nM for hTLR8, demonstrates anti-tumor properties and enhances the efficacy of PD-1/PD-L1 blockade treatments, making it valuable for cancer immunotherapy research [1].

TLR7/8 agonist 4 hydroxy-PEG6-acid, a drug-linker conjugate for antibody-drug conjugates (ADCs), comprises the TLR7/8 agonist 4 and a hydroxy-PEG6-acid linker, suitable for ADC synthesis [1].

Enpatoran is an inhibitor of TLR7(IC50 = 11.1 nM) and TLR8(IC50 = 24.1 nM). Enpatoran was found to be inactive against TLR3, TLR4, and TLR9 in vitro and in vivo.