Toll-like Receptors

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  1. TLR7 agonist

    Imiquimod (Aldara) is a a heterocyclic imidazoquinoline amide that acts as an immune response modifier.
  2. TLR7/8 Agonist

    Resiquimod is an immune response modifier that acts as a potent TLR 7/8 agonist. Phase 2.
  3. TLR Inhibitor

    TLR2-IN-C29 is an inhibitor of TLR2/1 and TLR2/6 signaling.
  4. TLR8 agonist

    VTX-2337 is a small-molecule Toll-like receptor 8 (TLR8) agonist with potential immunostimulating and antineoplastic activities.
  5. TLR7 agonist

    GS-9620 is a potent and selective orally active small molecule agonist of Toll-like receptor 7.
  6. TLR4 Inhibitor

    VGX-1027 displays immunomodulatory and anti-inflammatory activities by inhibiting toll-like receptor 4 (TLR4) signaling.
  7. TLR7 Ligand

    Toll-Like Receptor 7 Ligand II is a cell-permeable hydroxyadenine compound which acts as a potent and highly specific TLR7 (toll-like receptor 7) agonist without any detectable activity towards TLR2/3/5/8/9. It is shown to be 10-times more potent than R848 in stimulating the production of TLR7-dependent cytokines in cultures in vitro .
  8. MD2 inhibitor

    MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD of 189 ?μM for the recombinant human MD2 (rhMD2).
  9. TLR4 inhibitor

    Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor and plays pivotal role in various inflammatory diseases.
  10. TLR7 agonist

    PF-4878691 (3M-852A) is a potent, orally active, and selective Toll-like receptor 7 (TLR7) agonist modelled to dissociate its antiviral and inflammatory activities.
  11. Hydroxychloroquine Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
  12. TLR7 agonist

    Isatoribine is a novel guanosine analogue showing immunostimulatory activity both in vivo and in vitro.
  13. TLR7 agonist

    TLR7-agonist-2 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a LEC of 0.4 μM.

  14. TLR7 agonist

    Gardiquimod is a chemical compound which acts selectively at both mouse and human forms of toll-like receptor 7 (TLR7). It functions as an immune response modifier. CAS: 1159840-61-5 (TFA) 1020412-43-4 (free base)
  15. TLR/SCD inhibitor

    E6446 dihydrochloride is a robust antagonist for TLR7 and TLR9, with potential applications in studying harmful inflammatory responses. Additionally, it acts as a significant inhibitor of SCD1 with a KD of 4.61 μM. This compound can notably suppress adipogenic differentiation and liver lipogenesis via the SCD1-ATF3 pathway. Studies have indicated that E6446 dihydrochloride can enhance liver pathology in mice on a high-fat diet, making it a potential candidate for researching non-alcoholic fatty liver disease (NAFLD).

  16. MD2-TLR4 inhibitor

    MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively.
  17. TLR inhibitor

    AN-3485 is a benzoxaborole analog, Toll-Like Receptor(TLR) inhibitor with IC50 values ranging from 18 to 580 nM.
  18. TLR agonist

    CU-CPT17e is a potent multi-Toll-like receptor (TLR) agonist that activates TLR3, TLR8, and TLR9.
  19. TLR8 antagonist

    CU-CPT-9a is a specific TLR8 antagonist, with an IC50 of 0.5 nM.
  20. TLR7 agonist

    LHC-165 is a TLR7 agonist. Has potential to treat solid tumors.
  21. TLR1/2 inhibitor

    CU-CPT22 is a potent protein complex of toll-like receptor 1 and 2 (TLR1/2) inhibitor.
  22. human TLR2 antagonist

    MMG-11 is a potent and selective human TLR2 antagonist with low cytotoxicity.
  23. TLR7/8 agonist

    Telratolimod is a toll like receptors 7/8 (TLR7/8) agonist, with antitumor activity.
  24. TLR4 antagonist

    IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. It inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein.
  25. TLR7 agonist

    TLR7 agonist 1 is a potent, selective and oral TLR7 agonist with an IC50 of 90 nM.
  26. TLR8 antagonist

    CU-CPT9b is a specific TLR8 antagonist, with an IC50 of 0.7 nM. CU-CPT9b shows high binding affinity towards TLR8 with a Kd of 21 nM.
  27. TLR8 antagonist

    CU-CPT-8m is a specific TLR8 antagonist, with an IC50 of 67 nM.
  28. TLR4 Inhibitor

    S enantiomer of TAK-242. TAK-242 (Resatorvid), a small-molecule inhibitor of Toll-like receptor (TLR) 4 signaling. TAK-242 is in treatment of sepsis and septic shock.
  29. Toll-like receptors (TLRs) are a class of proteins that play a key role in the innate immune system.
  30. TLR7/8 agonist

    TLR7/8 agonist 1 dihydrochloride is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.
  31. TLR-9 Agonist

    ODN M362 is a class C oligodeoxynucleotide that acts as a TLR-9 agonist, promoting immune responses through the stimulation of toll-like receptor 9. This reagent is effective in inducing apoptosis in cancer cells, making it valuable for immunological studies and the development of therapeutic vaccines. Its application as a vaccine adjuvant enhances the efficacy of antigen-specific responses in research settings.
  32. TLR3 Agonist

    Polyinosinic-polycytidylic acid potassium is a synthetic analog of double-stranded RNA that acts as an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors. This reagent is utilized to stimulate innate and adaptive immune responses, serving as an effective vaccine adjuvant while also modifying the tumor microenvironment. Additionally, Polyinosinic-polycytidylic acid potassium can induce apoptosis in cancer cells, making it a valuable compound for cancer research and immunotherapy studies.
  33. TLR9 Inhibitor

    ODN 20844 is a TLR9 inhibitor designed to disrupt Toll-like receptor-mediated immune responses. As a guanine-modified inhibitory oligonucleotide, it specifically targets TLR7 and TLR9, leading to a reduction in immune cell activation. This compound is useful for research applications focused on modulating immune pathways and studying immune-related diseases. The sequence of ODN 20844 is 5'-TCCTGGCGc7GGGAAGT-3'.
  34. TLR7 Agonist

    TLR7 Agonist 3 acts as an effective agonist of Toll-like receptor 7 (TLR7), playing a significant role in the immune response modulation. This compound is utilized primarily in cancer research to explore its potential therapeutic effects in tumor immunity and the activation of anti-tumor responses. Its ability to stimulate TLR7 pathways makes it a valuable tool for investigating the mechanisms of immune activation and evaluating novel cancer treatments.
  35. TLR7/8 Agonist

    TLR7/8 Agonist 3 is a potent dual agonist of Toll-like receptors 7 and 8, designed to enhance the immune response against viral infections and tumors. This compound demonstrates significant biological activity through the activation of innate immune pathways, stimulating the production of pro-inflammatory cytokines. Research applications include immunotherapy and the study of host-pathogen interactions, making it a valuable tool for investigating TLR-mediated signaling and immune modulation.
  36. TLR7 Agonist

    BBIQ is an imidazoquinoline compound that acts as a potent and selective agonist for Toll-like receptor 7 (TLR7), exhibiting an EC50 of 59.1 nM in human TLR7. This compound serves as an effective vaccine adjuvant, significantly enhancing innate immune responses. BBIQ is valuable for research applications focused on immunology and vaccine development, facilitating the exploration of TLR7-mediated signaling pathways.
  37. TLR7 Agonist

    Imiquimod maleate is a selective toll-like receptor 7 (TLR7) agonist known for its immune response-modulating properties. It demonstrates significant antiviral and antitumor efficacy in vivo, making it a valuable compound in the study of various conditions. Research applications include the investigation of external genital and perianal warts, cancer, and COVID-19.
  38. TLR7 Agonist

    AZD8848 is a selective agonist of toll-like receptor 7 (TLR7) designed for research applications in asthma and allergic rhinitis. By activating TLR7, this compound enhances immune responses, making it a valuable tool for studying innate immunity and developing therapeutic strategies for related respiratory conditions.
  39. TLR7/8 Agonist

    TLR7/8 Agonist 4 is a potent agonist targeting Toll-like receptor 7 and 8. This compound enhances the activation of immune responses, exhibiting significant anti-cancer activity. Its efficacy makes it a promising tool for research in cancer immunotherapy and the study of innate immune signaling pathways.
  40. TLR8 Antagonist

    CU-115 is a potent TLR8 antagonist with an IC50 of 1.04 µM, demonstrating selectivity for TLR8 over TLR7 (IC50 > 50 µM). This compound effectively decreases the production of pro-inflammatory cytokines, including TNF-α and IL-1β, in R-848 activated THP-1 cells. CU-115 is suitable for research applications focusing on TLR8 signaling pathways and inflammatory responses.
  41. TLR7 Agonist

    E104 is a potent and selective TLR7 agonist that activates immune responses through Toll-like receptor 7. This compound enhances the activity of mouse macrophages and human peripheral blood mononuclear cells (hPBMCs), making it valuable in immuno-oncology research. E104's potential for use in antibody-drug conjugate (ADC) technology further supports its application in eliciting robust anticancer effects, contributing to the development of innovative cancer therapies.
  42. TLR7/TLR8 Inhibitor

    BMS905 is a potent dual inhibitor of Toll-like receptors 7 and 8, exhibiting IC50 values of 0.7 nM and 3.2 nM, respectively. This compound effectively inhibits IL-6 production induced by TLR7 or TLR8 activation in both human and mouse whole blood. BMS905 serves as a valuable tool for investigating the role of these receptors in autoimmune diseases, particularly lupus.
  43. TLR7/8 Agonist

    AXC-715 trihydrochloride is a dual agonist of Toll-like receptors 7 and 8 (TLR7/8). This compound enhances immune responses and can be utilized in the synthesis of antibody-adjuvant immunoconjugates, particularly for constructs targeting programmed death-ligand 1 (PD-L1). Its ability to stimulate TLR pathways makes AXC-715 a valuable tool for immunotherapy research and the development of therapeutic antibodies.
  44. TLR7 Agonist

    Bropirimine is an orally active Toll-like receptor 7 (TLR7) agonist. It has been shown to inhibit RANKL-induced osteoclast differentiation in mouse bone marrow-derived macrophages, highlighting its potential role in modulating bone metabolism. Additionally, Bropirimine exhibits dose-dependent inhibitory effects on colony formation in cultured KK-47 and 724 cells, making it a valuable tool for cancer research. This compound is relevant for studies investigating cancers and bone metabolic disorders such as osteoporosis.
  45. TLR7/8 Agonist

    PVP-037.2 is a TLR7/8 agonist that activates the immune response through the stimulation of Toll-like receptors. This compound enhances vaccine-induced TH1-type immune responses, leading to increased production of antigen-specific antibodies, particularly IgG1 and IgG2c. PVP-037.2 is valuable for research applications focused on immunology, vaccine development, and the modulation of adaptive immune responses.
  46. TLR7 Agonist

    SM-324405 is a potent TLR7 agonist with an EC50 of 50 nM, exhibiting pEC50 values of 7.3 for human TLR7 and 6.6 for rat TLR7. This compound is particularly useful in immunological research focused on allergic diseases. As an antedrug, SM-324405 is designed to be locally active and is rapidly metabolized to an inactive form upon systemic circulation, effectively mitigating the risk of systemic toxicity while maintaining agonistic activity in targeted environments.
  47. TLR Agonist

    3D-Monophosphoryl Lipid A-5 is a potent TLR agonist that enhances the immunogenicity of vaccines when used as an adjuvant. This compound stimulates innate immune responses, promoting the activation of various immune cells and cytokine production. It is valuable in research applications focused on vaccine development and immunotherapy, offering insights into the modulation of immune responses.
  48. TLR8 Agonist

    TLR8 agonist 5 is a potent agonist of Toll-like receptor 8 (TLR8), demonstrated by an EC50 of 20 nM in the HEK-Blue hTLR8 cell line. This compound effectively stimulates the immune response, making it a valuable tool for research in immunology and inflammation studies. Its ability to activate TLR8 highlights its potential applications in therapeutic development targeting immune-related pathways.
  49. TLR7 Agonist

    1V209 is a Toll-like receptor 7 (TLR7) agonist that exhibits anti-tumor effects through the activation of the TLR7 signaling pathway. This compound can be conjugated with various polysaccharides to enhance its water solubility, thereby improving its efficacy while maintaining low toxicity. 1V209 is suitable for research applications aimed at understanding immune responses and developing cancer immunotherapies.
  50. TLR Inhibitor

    ODN 24991, a guanine-modified inhibitory oligonucleotide, functions as an inhibitor of Toll-like receptors TLR3, TLR7, and TLR9. By disrupting TLR-mediated immune cell signaling, ODN 24991 serves as a valuable tool for investigating immune responses. The compound is particularly useful in research aimed at understanding the role of these TLRs in inflammation and immune regulation. ODN 24991 sequence: 5'-C-C-T-G-G-C-c7rGm-G-G-G-3'.

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