Catalog No.
Product Name
Application
Product Information
Citations
-
TLR7 Agonist
AZ12441970 is a potent and selective agonist of Toll-like receptor 7 (TLR7), demonstrating pEC50 values of 6.8 and 6.6 for human and rat TLR7, respectively. This compound exhibits efficacy in a mouse model of allergic airway disease, while inducing minimal systemic IFN-α levels. AZ12441970 serves as a valuable tool for research into allergic airway conditions and TLR7-mediated immune responses. -
TLR Agonist
Monophosphoryl lipid A free acid acts as a toll-like receptor 4 (TLR4) agonist, stimulating innate immune responses. Derived from the cell wall of nonpathogenic Salmonella, this compound is relevant for research into immunization and vaccine development. Its ability to activate TLR4 makes it a valuable tool for studying immune modulation and potentially enhancing vaccine efficacy. -
TLR7 Agonist
TLR7 Agonist 14 (compound 17b) is a potent activator of Toll-like receptor 7 (TLR7) with an EC50 value of 18 nM. This compound effectively stimulates the activation of mouse macrophages and human peripheral blood mononuclear cells (hPBMCs) at low nanomolar concentrations. Its significant biological activity makes it a valuable tool for research applications focused on immune modulation and inflammation pathways. -
TLR7/8 Agonist
UM-3006 is a potent TLR7/8 agonist that activates Toll-like receptor signaling pathways to enhance immune responses. This compound exhibits significant biological activity in promoting adaptive and innate immunity, making it a valuable tool for research applications focused on vaccine development and the study of immune-related diseases. Its potential as a vaccine adjuvant further underscores its relevance in immunological studies. -
TLR4/JNK/NF-κB Inhibitor
TLR4-IN-2 is an inhibitor targeting TLR4, JNK, and NF-κB pathways. It demonstrates anti-inflammatory properties by reducing nitric oxide production in LPS-stimulated RAW264.7 cells, with an IC50 of 23.2 µM. By inhibiting TLR4 expression and diminishing JNK phosphorylation, TLR4-IN-2 effectively suppresses NF-κB activation and the transcription of inflammation-related genes, leading to lower levels of iNOS, COX-2, and various inflammatory mediators. This compound shows potential for investigating therapeutic strategies in inflammatory diseases such as rheumatoid arthritis and other inflammatory disorders. -
TLR8 Agonist
TLR8 Agonist 10 is a selective agonist targeting Toll-like receptor 8 (TLR8), demonstrating an EC50 of 0.019 μM in human cells. This compound activates TLR8-mediated signaling pathways, functioning as a latency-reversing agent that reactivates latent HIV-1 reservoirs. Additionally, TLR8 Agonist 10 enhances the activity of innate cytotoxic natural killer cells, allowing for targeted effects on HIV-infected CD4+ T cells. This reagent is valuable for research focused on HIV-1 infection and immune modulation. -
TLR4 Agonist
3D-Monophosphoryl Lipid (14) is a potent TLR4 agonist that acts to stimulate the immune response. This compound serves as an effective vaccine adjuvant, enhancing the immunogenicity of various vaccine formulations. Its applications in research include the development of improved vaccines and studying immune system activation pathways. -
TLR7 Agonist
AYK004-B1 is a potent TLR7 agonist with an EC50 of 0.2265 nM. This compound enhances immune responses and is suitable for the development of immune adjuvants in various research applications. Its ability to modulate Toll-like receptor pathways makes it valuable for studies in immunology and vaccine development. -
TLR7 Agonist
Imiquimod dihydrochloride is a selective TLR7 agonist, known for its role as an immune response modifier. It exhibits significant antiviral and antitumor activities in vivo, making it a valuable tool in research. This compound is applicable in the investigation of external genital and perianal warts, cancer therapies, and potential responses to COVID-19. -
TLR Inhibitor
IMG-2005 is a Toll-like receptor (TLR) inhibitor that disrupts TLR signaling by mimicking the Toll/interleukin-1 receptor (TIR) domain of MyD88. This mechanism prevents the homodimerization of MyD88, mitigating damage to tracheal epithelial cells and reducing the onset of pulmonary immune diseases. IMG-2005 is valuable for research into TLR-related pathways and the development of therapeutic strategies for respiratory inflammation. -
TLR7 Agonist
TLR7 Agonist 22 selectively targets Toll-like receptor 7 (TLR7) with an IC50 of 25.86 μM. This compound effectively inhibits the secretion of HBsAg in cells while robustly activating TLR7, resulting in the induction of cytokines such as IL-12, TNF-α, and IFN-α in human peripheral blood mononuclear cells (PBMCs). TLR7 Agonist 22 holds potential for research focused on the development of novel immunomodulatory agents for hepatitis B virus (HBV) therapy. -
TLR4 Antagonist
CRX-526 is a TLR4 antagonist that inhibits the interaction of lipopolysaccharide (LPS) with immune cells, effectively reducing the expression of pro-inflammatory genes and the release of TNF-α induced by LPS. This compound demonstrates significant anti-inflammatory properties, as evidenced by its efficacy in two distinct mouse models of colitis: the dextran sodium sulfate-induced colitis model and the multidrug resistance gene 1a-deficient model. CRX-526 is a valuable tool for research focused on inflammatory pathways and associated therapeutic interventions. -
TLR7/8 Agonist
AYK004 is a TLR7/8 agonist that stimulates immune responses through the activation of the Toll-like receptor signaling pathway. As an adenine derivative with an optimized hydrophilic-lipophilic balance, AYK004 enhances loading capacity and stability in immunoadjuvant systems, such as liposomes. This compound is particularly useful for research applications focused on innate immunity and the development of vaccine adjuvants, while minimizing potential side effects associated with systemic immunity. -
TLR4/MD2 Ligand
1Z105 is a potent TLR4/MD2 ligand, known for its oral bioactivity. This compound promotes dendritic cell maturation and enhances antigen presentation, making it a valuable tool for studying immune responses. Additionally, 1Z105 has demonstrated therapeutic potential in preventing arthritis, contributing to research in autoimmune disease modulation and immune system regulation. -
TLR Agonist
AYK004-C1 is a Toll-like receptor (TLR) agonist that plays a crucial role in modulating immune responses. This compound is utilized in the development of immune adjuvants, enhancing the efficacy of vaccines and therapeutic agents. Its ability to activate TLR pathways makes it an important reagent for research in immunology and vaccine development. -
TLRs Activator
Creatine ethyl ester (CEE) serves as an activator of Toll-like receptors (TLRs), specifically TLR2, TLR3, TLR4, and TLR7. This compound is notable for its short-term capability to upregulate these receptors, making it a valuable tool in immunological research. Its role in modulating TLR activity may provide insights into innate immune responses and their implications in various disease contexts. -
TLR7/8 Agonist
TLR7/8 Agonist 13 is a potent dual agonist targeting Toll-like receptors 7 and 8, with lowest effective concentrations (LEC) of 1.6 μM for both human receptors. This compound demonstrates significant biological activity by stimulating human peripheral blood mononuclear cells (hPBMCs) at an LEC of 0.5 μM, leading to the induction of endogenous interferon-alpha (IFNα). In preclinical models, TLR7/8 Agonist 13 enhances the activation of myeloid dendritic cells and monocytes towards a TH1 phenotype and reduces viral load as well as Hepatitis B virus (HBV) surface antigen expression. It serves as a valuable tool for investigating immune responses in HBV-related research. -
TLR Agonist
3D-Monophosphoryl Lipid A-5 free acid is a Toll-like receptor (TLR) agonist known for its potential to enhance immune responses. This compound serves as an effective vaccine adjuvant, bolstering the immunogenicity of various vaccine formulations. Its application in research focuses on elucidating immune mechanisms and improving vaccine efficacy. -
TLR7/8 Adjuvant
AYK005 is a potent TLR7/8 agonist that enhances the immune response by activating innate immune signaling pathways. Its primary mechanism involves stimulation of Toll-like receptor 7 and 8, leading to increased production of pro-inflammatory cytokines and promotion of adaptive immunity. AYK005 is utilized in research applications focused on vaccine development and immunotherapy, offering insights into TLR-mediated immune modulation. -
TLR9 Agonist
Agatolimod sodium, a TLR9 agonist, is classified as a class B CpG oligodeoxynucleotide (ODN 2006). It enhances immune responses and is widely utilized as a vaccine adjuvant. In addition, Agatolimod sodium serves as a valuable tool in cancer research, aiding studies aimed at understanding tumor immunology. Sequence: 5’-TCGTCGTTTTGTCGTTTTGTCGTT-3’. -
TLR7/8 Inhibitor
Enpatoran is a potent and orally active dual inhibitor of Toll-like receptors 7 and 8, exhibiting IC50 values of 11.1 nM and 24.1 nM, respectively, in HEK293 cells. This compound is selective, showing no activity against TLR3, TLR4, or TLR9. Enpatoran effectively blocks both synthetic and natural RNA ligands, demonstrating excellent pharmacokinetic properties in vivo. It is a valuable tool for research focused on modulating innate and adaptive immune responses related to autoimmunity. -
TLR3 Inhibitor
CU-CPT 4a is a selective inhibitor of TLR3 signaling, effectively blocking the downstream pathways activated by the TLR3/dsRNA complex. This compound suppresses the production of pro-inflammatory cytokines, including TNF-α and IL-1β, making it a valuable tool for research into immune responses and inflammation. CU-CPT 4a is suitable for studies focused on modulating TLR3-related signaling pathways in various disease models. -
TLR7 Agonist
Imiquimod hydrochloride is a selective TLR7 agonist that serves as an immune response modifier. It demonstrates notable antiviral and antitumor properties in vivo, making it a valuable tool for studying various conditions. Research applications include exploration of treatments for external genital and perianal warts, cancer therapies, and potential therapeutic approaches for COVID-19. -
TLR2 Agonist
Zymosan A is a TLR2 agonist derived from Saccharomyces cerevisiae, known for its ability to activate Toll-like receptor 2. It demonstrates significant radioprotective effects, effectively mitigating ionizing radiation-induced intestinal injuries in murine models. Additionally, Zymosan A supports the regeneration of intestinal stem cells following radiation exposure, making it a valuable tool for research in intestinal health and radioprotection. -
TLR9 Ligand
ODN 2216 is a selective agonist for human Toll-like receptor 9 (TLR9), known for its role in immune modulation. It stimulates the production of large quantities of interferons, specifically IFN-α and IFN-β, through activation of plasmacytoid dendritic cells (pDCs). ODN 2216 also enhances IL-12 (p40) production by dendritic cells and promotes interferon-gamma (IFN-γ) secretion in peripheral blood mononuclear cells (PBMC) in an indirect manner mediated by IFN-α/β. Additionally, this reagent activates natural killer (NK) cells and supports IFN-γ production in TCR-activated CD4+ T cells, making it valuable for research in immunology and vaccine development. -
TLR Antagonist
ODN TTAGGG is a TLR9, AIM2, and cGAS antagonist that functions as an inhibitory oligonucleotide. This compound inhibits the activation of the AIM2 inflammasome as well as cGAS by competing with endogenous DNA. As a result, ODN TTAGGG obstructs AIM2-mediated pyroptosis and reduces IL-18 production. Its immunosuppressive properties make it useful in research related to autoimmune diseases, including lupus erythematosus. -
TLR7/TLR9 Inhibitor
AT791 is a potent inhibitor of Toll-like receptors 7 and 9 (TLR7/TLR9), demonstrating strong oral bioavailability. This compound effectively blocks TLR7 and TLR9 signaling pathways in a range of human and murine cell types, as well as inhibiting DNA-TLR9 interactions in vitro. AT791 is applicable in research focused on immune modulation and the characterization of TLR-mediated signaling. -
TLR3/7/9 Inhibitor
ODN 2088 is a potent inhibitor of Toll-like receptors 3, 7, and 9 (TLR3, TLR7, TLR9), demonstrating a strong capacity to modulate immune responses. This compound effectively suppresses the release of key pro-inflammatory cytokines, including interferon-alpha (IFN-α) and interleukin-6 (IL-6), without exhibiting cytotoxic effects. ODN 2088 is valuable for research applications focused on understanding TLR-mediated signaling pathways and their roles in various immune-related conditions. -
TLR2/TLR4 Antagonist
Sparstolonin B is a selective antagonist of Toll-like receptors 2 and 4 (TLR2/TLR4), effectively inhibiting TLR2- and TLR4-mediated inflammatory signaling pathways. This compound demonstrates notable anti-HIV and anticancer properties, making it valuable for research into immune modulation and cancer therapy. Its ability to block key inflammatory responses adds significance to its use in studying various diseases linked to TLR signaling. -
TLR9 Agonist
ODN 2395 is a C class oligodeoxynucleotide that functions as a TLR9 agonist, promoting immune responses. Its primary application is as a vaccine adjuvant, enhancing the efficacy of immunological vaccines. This compound facilitates the activation of dendritic cells and B cells, thereby driving robust adaptive immunity. Sequence: 5'-tcgtcgttttcggcgc:gcgccg-3'. -
TLR9 Agonist
ODN 1018 is a Toll-like receptor 9 (TLR9) agonist functioning as an immune modulator. It demonstrates adjuvant activity by enhancing CD8+ T cell responses when combined with liposomal nanoparticles encapsulating ovalbumin (OVA) peptides. Additionally, ODN 1018 effectively induces prolonged suppression of allergic airway inflammation, making it a valuable tool for research into allergic asthma and systemic lupus erythematosus. -
Toll-like Receptor (TLR) Inhibitor
Okanin is a potent Toll-like Receptor (TLR) inhibitor derived from the flowering plant Coreopsis tinctoria. It exhibits significant biological activity by attenuating lipopolysaccharide (LPS)-induced microglial activation via the inhibition of the TLR4/NF-κB signaling pathway. This compound is useful for research applications focusing on neuroinflammation and the modulation of immune responses in microglial cells. -
TLR7/8 Inhibitor
Enpatoran hydrochloride is a dual inhibitor of Toll-like receptors 7 and 8, demonstrating potent activity with IC50 values of 11.1 nM and 24.1 nM, respectively, in HEK293 cells. This compound is selectively inactive against TLR3, TLR4, and TLR9, effectively blocking both synthetic and natural RNA ligands. Enpatoran hydrochloride exhibits favorable pharmacokinetic profile in vivo, making it a valuable tool for research into innate and adaptive autoimmunity pathways. -
TLR7/8 Agonist
CL097 is a potent agonist of Toll-like receptors 7 and 8 (TLR7/8), eliciting a robust pro-inflammatory cytokine response in macrophages. By priming NADPH oxidase, CL097 enhances fMLF-stimulated reactive oxygen species (ROS) production. This compound is valuable for research applications in immunology and inflammation studies, particularly in understanding innate immune responses. -
TLR9 Inhibitor
TLR9-IN-1 is a potent and selective inhibitor of Toll-like receptor 9 (TLR9), exhibiting an IC50 value of 7 nM for human TLR9. This compound is valuable for studying diseases linked to aberrant immune responses, making it an important tool in immunological research and therapeutic development. Researchers can utilize TLR9-IN-1 to explore the modulation of TLR9 pathways in various inflammatory and autoimmune conditions. -
TLR8 Agonist
Selgantolimod is a potent and selective agonist of toll-like receptor 8 (TLR8). This orally active compound has demonstrated significant biological activity in activating the immune response, making it a valuable agent in the treatment of hepatitis B virus (HBV) and human immunodeficiency virus (HIV) infections. Its mechanism of action supports research into immunotherapeutic strategies targeting viral pathogens. -
TLR7/8 Agonist
Gardiquimod is an imidazoline compound that acts as an agonist for Toll-like receptors 7 and 8 (TLR7/8). This reagent has been shown to inhibit HIV-1 infection in macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 at concentrations below 10 μM, making it a valuable tool in immunological research and studies related to viral infections. -
TLR8 Agonist
TL8-506 is a selective TLR8 agonist with an EC50 of 30 nM. This compound exhibits immunomodulatory properties, making it a valuable tool for investigating therapeutic approaches in tuberculosis and cancer immunotherapy. Researchers can leverage TL8-506 to enhance immune responses and study the underlying mechanisms of TLR8-mediated signaling. -
TLR-9 Agonist
ODN 1668 is a TLR-9 agonist classified as a class B CpG oligodeoxynucleotide (ODN). This reagent exhibits significant immune regulatory properties, enhancing IgG2 antibody levels and promoting T cell and B cell immune responses, making it useful in vaccine adjuvant research. Additionally, ODN 1668 induces an antimicrobial immune response through a CaTLR9-dependent pathway in groupers. Sequence: 5'-tccatgacgttcctgatgct-3’. -
Toll-like Receptor (TLR) Agonist
TLR7/8 Agonist 1 is a dual agonist of Toll-like Receptors 7 and 8, belonging to the imidazoquinoline class. This compound activates the innate immune response by engaging TLR7 and TLR8, leading to the production of pro-inflammatory cytokines. It has significant applications in immunological research, particularly in studies related to viral infections, cancer immunotherapy, and the modulation of immune responses. -
TLR7/TLR8 Inhibitor
TLR7/8-IN-1 is a potent inhibitor of Toll-like receptors 7 and 8, which play critical roles in the immune response. This compound exhibits strong potential in modulating inflammatory pathways associated with autoimmune diseases. It serves as a valuable tool for researchers investigating the therapeutic targeting of TLR7 and TLR8 in various immunological studies. -
Toll-like Receptor (TLR) Agonist
Neoseptin 3 is an agonist of Toll-like receptor 4 (TLR4) and myeloid differentiation factor 2 (MD-2), exhibiting an EC50 of 18.5 μM. This compound promotes innate immune responses and enhances cytokine production, making it a valuable tool for studying immune system activation. Neoseptin 3 is suitable for research on inflammatory diseases and immune modulation. -
TLR8 Agonist
CL075 is a selective TLR8 agonist that activates the MyD88-dependent signaling pathway, leading to the production of inflammatory cytokines and type I interferons (IFNs). This compound enhances NF-κB and IRF7 activation, contributing to immune modulation. It is primarily used in research applications focused on inflammation and immune response mechanisms. -
TLR3 Ligand
Polyinosinic acid sodium is the sodium salt of polyinosinic acid, a single-stranded homonucleic acid that serves as a Toll-like Receptor 3 (TLR3) ligand. By activating TLR3, polyinosinic acid sodium enhances the cellular immune response through the TRIF signaling pathway. This reagent shows potential for use in studies focused on immune regulation and adjuvant therapies in various research applications. -
TLR4 Inhibitor/PROTAC Linker
TLR4-IN-C34-C2-COOH is a TLR4 inhibitor that serves as a PROTAC linker. It demonstrates significant potential in the modulation of inflammatory responses, particularly in studies involving acute myocardial injury. By targeting TLR4 in enterocytes and macrophages, TLR4-IN-C34-C2-COOH effectively reduces systemic inflammation in murine models of endotoxemia and necrotizing enterocolitis, making it a valuable tool for research in inflammation-related pathways. -
TLR 7 Agonist
Loxoribine, a guanosine analog, functions as a selective Toll-like receptor (TLR) 7 agonist. This compound exhibits significant anti-viral and anti-tumor activities, making it valuable for research applications in immunotherapy and cancer treatment. Its oral bioavailability expands its potential for in vivo studies. -
TLR7 Agonist
DSR-6434 is a highly potent and selective agonist of Toll-like receptor 7 (TLR7), exhibiting EC50 values of 7.2 nM for human TLR7 and 4.6 nM for mouse TLR7. This compound demonstrates significant antitumor activity, making it a valuable tool for studying cancer immunotherapy and TLR7 signaling pathways in various research applications. -
TLR7 Agonist
CL264 is a selective agonist of Toll-like receptor 7 (TLR7), primarily utilized for examining innate immune signaling pathways. This compound enhances the activation of immune responses through TLR7 stimulation, making it a valuable tool for research in immunology and inflammation. Its application extends to understanding the mechanisms of antiviral responses and potential therapeutic strategies targeting TLR-mediated immune modulation. -
Toll-like Receptor (TLR) Antagonist
TLR7/8/9-IN-1 is a potent small molecule antagonist targeting Toll-like receptors 7, 8, and 9, with an IC50 value of 43 nM. This compound effectively inhibits TLR-mediated signaling pathways, playing a crucial role in the immune response. It is valuable for research applications focused on inflammatory diseases, autoimmune disorders, and the modulation of innate immunity. -
TLR9 Agonist
CpG ODN 10101 is a TLR9 agonist, designed as a synthetic oligodeoxynucleotide modified with phosphate thioester. This compound activates B cells and plasmacytoid dendritic cells, leading to enhanced production of cytokines and chemokines, including interferon-α and IP-10. By modulating innate immunity and promoting Th1 adaptive responses, CpG ODN 10101 demonstrates antiviral properties and enhances vaccine immunogenicity, highlighting its potential as an immunomodulator and vaccine adjuvant in the development of therapies for chronic hepatitis C and various infectious diseases.
