TLR7 Agonist

Guretolimod (DSP-0509) is a Toll-like receptor 7 (TLR7) agonist.

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

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).

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.

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.

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.

TLR7 agonist 20 is a selective Toll-like receptor 7 (TLR7) agonist with an EC₅₀ of 0.22 μM. TLR7 agonist 20, 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 can be used in studies related to non-inflammatory potent vaccine adjuvants.

TLR7 agonist 28 (compound 3) is a potent TLR7 agonist. TLR7 agonist 28 can conjugat to antitumor monoclonal antibodies (mAbs) for cancer immunotherapy.

TLR7 agonist 29 (Compound 1) is the agonist for TLR7 with an EC₅₀ of 5.2 nM for human TLR7 (EC₅₀ for mouse TLR7 is 48.2 nM). TLR7 agonist 29 activates bone marrow-derived macrophages (BMDMs), stimulates myeloid cells in the tumor microenvironment, promotes the expression of PD-L1, CD86 and IFN-α. TLR7 agonist 29 can be used as payload for synthesis of ADC.

TLR7 agonist 7 (compound IIb-26) is an TLR7 agonist with an EC₅₀ value of ~4 nM.

TLR7 agonist 24 (Compound 21) is an agonist for TLR7 with EC₅₀ of 3.72 μM. TLR7 agonist 24 can be used as a vaccine adjuvant when combined with Aluminum Hydroxide (HY-B1521), that enhances the immune response against SARS-CoV-2 and hepatitis B antigens.

AYK004-B1 is a TLR7 agonist (EC₅₀=0.2265 nM). AYK004-B1 can be used to prepare immune adjuvants.

TLR7/8 agonist 14 is a TLR7 and TLR8 agonist with EC₅₀ values of 0.53 μM and 4.3 μM, respectively. TLR7/8 agonist 14 increases the secretion of the proinflammatory cytokines TNF-α, IL-1β, IL-8 and IFN-γ. TLR7/8 agonist 14 increases cytokine secretion and expression of CD86. LR7/8 agonist 14 can be used for research colorectal carcinoma.

TLR7 agonist 9 (compound 10) is an aonist of TLR7. TLR7 agonist 9 can be used for research of cancer and infectious disease. TLR7 agonist 9 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

TLR7 agonist 27 (compound 24) is a potent TLR7 agonist with an EC₅₀ of 238.1 nM. TLR7 agonist 27 shows weak agonistic activity against NOD2 (nucleotide-binding oligomerization domain 2) (EC₅₀ of 6.2 μM). TLR7 agonist 27 is a potent immunostimulant, and can be used as a vaccine adjuvant and/or immunotherapeutic.

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

TLR7 agonist 5 (compound IIb-11) is an TLR7 agonist with an EC₅₀ value of ~4 nM.