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TLR Agonists

Cat.No. Product Name Information Product Use Citations Product Validations
S8133 Resiquimod (R-848) Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist, inducing the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. This compound reduces hepatitis C virus (HCV) infection. Phase 2.
Nature, 2025, 644(8078):1058-1068
J Virol, 2025, e0128025.
Int J Nanomedicine, 2024, 19:3589-3605
S7161 Motolimod Motolimod is a selective and potent Toll-like receptor 8 (TLR8) agonist with EC50 of 100 nM, > 50-fold selectivity over TLR7. Phase 2.
Journal of Leukocyte Biology, 2025, qiaf036
J Leukoc Biol, 2025, 117(5)qiaf036
J Pharmacol Exp Ther, 2024, 388(3):751-764
S7221 Vesatolimod (GS-9620) Vesatolimod (GS-9620) is a potent and selective orally active small molecule agonist of Toll-like receptor 7.
PLoS Pathog, 2022, 18(3):e1010354
J Pharm Biomed Anal, 2020, 179:112987
Stem Cell Res Ther, 2019, 10(1):387
S0078 1V209 (TLR7 agonist T7) 1V209 (TLR7 agonist T7) is an agonist of Toll-like receptor 7 (TLR7) with anti-tumor effects. It can be used as vaccine adjuvants and enhances antigen specific humoral and cellular immune responses.
Acta Pharmaceutica Sinica B, 2024, 4577-4590
Acta Pharm Sin B, 2024, 14(10):4577-4590
Nano Letters, 2021, 7960–7969
S2979 CU-T12-9 CU-T12-9 is a specific agonist of Toll-like receptor (TLR) 1/2 with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. This compound activates both the innate and the adaptive immune systems. It signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.
Nat Commun, 2025, 16(1):2743
Biomedicine & Pharmacotherapy, 2023, 114638
Biomed Pharmacother, 2023, 162:114638
E0518 Poly(I:C) (Polyinosinic-Polycytidylic Acid) Polyinosinic acid-polycytidylic acid (Polyinosinic-polycytidylic acid; Poly(I:C)), a double-stranded RNA that induces innate immunity in mammals, is a candidate immunopotentiator for pharmaceuticals. Polyinosinic acid-polycytidylic acid is dsRNA formed by the long chain decomposition of muscle poly (I) homopolymer into poly (C) homopolymer.
J Hepatocell Carcinoma, 2023, 10:697-712
S0494 SM 324405 SM 324405 (compound 9e) is a potent and selective Toll-like receptor 7 (TLR7) agonist with EC50 of 50 nM.
E6040 Imiquimod maleate Imiquimod maleate (R 837 maleate) is a small-molecule salt derivative of maleic acid, isolated from the Imiquimod free base and is an immune response modifier, a potent and selective agonist of toll like receptor 7 (TLR7), an antagonist of adenosine A₂A receptor with a Ki of 2.16 μM, and an inhibitor of adenylyl cyclase activity, inducing antiviral proteins like cystatin A. It exhibits strong antitumoral and antiviral efficacy, making it effective for conditions such as COVID 19, HPV warts, molluscum contagiosum, actinic keratosis, basal and squamous cell carcinoma, Bowen's disease, and vulvar intraepithelial neoplasia.
S8428 FSL-1 FSL-1, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection.
S8827New Diprovocim Diprovocim is a potent synthetic agonist that activates the human TLR1/TLR2 heterodimer with an EC50 of 110 pM in THP-1 cells. It also exhibits significant potential as an immune adjuvant.
E5893New MTT5 MTT5 is an agonist of TLR7 that activates dendritic cells and CD8⁺ T cells, enhancing immune responses in the tumor microenvironment. When linked to an ADC, it enhances antitumor efficacy through combined immune stimulation and cytotoxicity.
S9623 Telratolimod (3M-052) Telratolimod (3M-052, MEDI9197) is an agonist of toll-like receptor 7 (TLR-7) and toll-like receptor 8 (TLR-8) with antitumor activity.
E0639 TLR7/8 agonist 1 dihydrochloride TLR7/8 agonist 1 dihydrochloride is a toll-like receptor TLR7/TLR8 dual-agonistic imidazoquinoline.TLR7/8 agonist 1 retains TLR7-agonistic activity with an EC50 of 20 nM.
E6039 Imiquimod hydrochloride Imiquimod hydrochloride (R 837 hydrochloride) is a small-molecule immune response modifier, a potent and selective agonist of toll like receptor 7 (TLR7), an antagonist of adenosine A₂A receptor with a Ki of 2.16 μM, and an inhibitor of adenylyl cyclase activity, inducing antiviral proteins like cystatin A. It exhibits strong antitumoral and antiviral efficacy, making it effective for conditions such as COVID 19, HPV warts, molluscum contagiosum, actinic keratosis, basal and squamous cell carcinoma, Bowen's disease, and vulvar intraepithelial neoplasia.
E7472 Pam3CSK4 Pam3CSK4 (Pam3Cys-Ser-(Lys)4) is a synthetic triacylated lipopeptide that serves as a ligand for the Toll-like receptor 2/1 (TLR2/1) heterodimer. It is an agonist of toll-like receptor 1/2 (TLR1/2) with an EC50 of 0.47 ng/mL in human TLR1/2.
E5909New CL075 CL075 (3M002) is a selective agonist of TLR8 with immunomodulatory properties. It primes human neutrophils by activating signaling pathways, including p47phox phosphorylation and p38MAPK, leading to enhanced reactive oxygen species (ROS) production and contributing to immune defense.
P1246 ODN 1826 sodium (CpG 1826 sodium) ODN 1826 sodium (CpG 1826 sodium) is a synthetic CpG oligodeoxynucleotide and agonist of TLR9 signaling pathway, that induces G1-phase arrest and apoptosis in A20 lymphoma cells while stimulating NO and iNOS production in mouse models, as part of its immunostimulatory activity.
E7559 RS 09 RS09 is a synthetic peptide mimic of Lipopolysaccharide (LPS) that serves as an agonist of TLR4. It activates TLR4, leading to NF-κB activation and inflammatory cytokine release, thereby enhancing immune responses. It also exhibit potential as an adjuvant by promoting antigen-specific antibody production in vivo.