Catalog No.
Product Name
Application
Product Information
Citations
-
TLR7/8 Agonist
m-AM-BBIQ is a dual agonist for Toll-like receptors 7 and 8 (TLR7/8), exhibiting EC50 values of 0.12 μM and 1.7 μM for human TLR7 and TLR8, respectively. This compound elicits strong immune responses, making it a valuable tool in immunology research and vaccine development. Its ability to activate TLR7/8 pathways can facilitate studies on innate immune activation and the potential enhancement of antiviral responses. -
TLR7/8 Agonist
Gardiquimod hydrochloride is a potent TLR7/8 agonist that activates the immune response. It has been shown to inhibit HIV-1 infection in macrophages and effectively activates peripheral blood mononuclear cells (PBMCs). This compound selectively stimulates TLR7 at concentrations below 10 μM, making it a valuable tool for research in immunology and antiviral therapy. -
TLR7 Agonist
TLR7 Agonist 8 (compound IIb-34) selectively activates Toll-like receptor 7 (TLR7) with an EC50 of approximately 4 nM. This potent agonist stimulates immune responses and plays a critical role in enhancing antiviral and antitumor immunity. It is valuable for research applications related to immunology and the development of therapeutics targeting TLR7 pathways. -
TLR7 Agonist
TLR7 Agonist 15 is a potent TLR7 activator that exhibits an EC50 of 18 nM. This compound effectively stimulates the activation of mouse macrophages and human peripheral blood mononuclear cells (hPBMCs) at low nanomolar concentrations. It holds potential applications in immunology research, particularly in studies focused on innate immune responses and antiviral mechanisms. -
Toll-like Receptor (TLR) Inhibitor
Tilsotolimod is a synthetic agonist of Toll-like receptor 9 (TLR9) involved in modulating immune responses. It has exhibited significant antitumor activity in preclinical models, making it a valuable reagent for cancer immunotherapy research. This compound is utilized in studies focused on enhancing the immune system's ability to target and eradicate tumors. -
TLR-9 Agonist
Cobitolimod sodium is a TLR-9 agonist that exhibits anti-inflammatory properties through its action on immune signaling pathways. This DNA oligonucleotide effectively inhibits Th17 cell activation while enhancing the expression of the anti-inflammatory markers FoxP3 and IL-10. By targeting and inhibiting the IL-17 signaling pathway, Cobitolimod sodium is valuable for research focused on inflammatory diseases and immune modulation. -
TLR4 Activator
CCL-34 is a potent Toll-like receptor 4 (TLR4) activator that effectively promotes dendritic cell maturation by significantly increasing CD83 expression and IL-12p70 production in a dose-dependent manner. This compound enhances the allostimulatory capacity of dendritic cells, leading to increased proliferation and IFN-γ secretion in naive CD4+CD45+RA+ T cells. Additionally, CCL-34 has demonstrated its capacity to boost antigen presentation in murine models with doxorubicin-treated colorectal cancer cells, making it valuable for research into immune stimulation and therapeutic strategies. -
TLR7/8 Agonist
TLR7/8 Agonist 9 is a potent agonist of Toll-like receptors 7 and 8, exhibiting EC50 values of 40 nM and 23 nM, respectively, for human TLR7 and TLR8. This compound demonstrates anti-tumor activity and enhances the efficacy of PD-1/PD-L1 blockade, making it a valuable tool for cancer immunotherapy research. It is suitable for studies investigating immune modulation and therapeutic strategies in oncological applications. -
TLR7 Agonist
TLR7 Agonist 33 is a potent activator of Toll-like receptor 7 (TLR7) with an EC50 of 1 nM. This compound exhibits significant immunostimulatory activity, making it suitable for cancer research and therapeutic applications targeting TLR signaling pathways. Its ability to enhance innate immune responses positions TLR7 Agonist 33 as a valuable tool in studying the role of TLR7 in tumor immunity and potential cancer treatments. -
TLR7/8 Antagonist
TLR7/8 Antagonist 1 is a potent antagonist of Toll-like receptors 7 and 8, exhibiting IC50 values of 3.91 μM and 2.19 μM, respectively. This imidazoquinoline derivative is instrumental in modulating immune responses and serves as a valuable tool in research applications targeting infectious diseases, cancer, and autoimmune disorders. Its unique mechanism of action enables the exploration of TLR-mediated pathways, contributing to the development of novel immunomodulatory therapies. -
TLR-9 Agonist
Cobitolimod is a TLR-9 agonist that exhibits anti-inflammatory activity through the modulation of immune responses. It effectively suppresses Th17 cell activity while promoting the expression of anti-inflammatory markers such as FoxP3 and IL-10. This action inhibits the IL-17 signaling pathway, making Cobitolimod valuable for research investigating inflammatory diseases and immune regulation mechanisms. -
TLR7 Agonist
TLR7 Agonist 26 is a potent agonist of Toll-like receptor 7 (TLR7), exhibiting an EC50 value of 225.5 nM. This compound demonstrates significant immunopotentiating effects, making it a valuable tool in immunological research. It is suitable for studies focused on enhancing immune responses and investigating TLR7-mediated pathways in various biological contexts. -
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. -
NLRP3 Inflammasome Inhibitor
(rac)-NDT-19795 is a potent inhibitor of the NLRP3 inflammasome, exhibiting an IC50 value of 66 nM in peripheral blood mononuclear cells (PBMCs) and 4.7 μM in Western blot assays. This racemic compound is derived from NT-0796 and possesses carboxylic acid activity, facilitating intracellular conversion. (rac)-NDT-19795 is valuable for investigating the mechanisms of inflammation and neurological disorders. -
Antacid Aegnt
Aluminum Hydroxide is a well-known antacid agent that functions primarily as an adjuvant in vaccine formulations. It enhances the immune response by promoting the pro-phagocytic effect and activating the pro-inflammatory NLRP3 pathway. Additionally, Aluminum Hydroxide compensates for the low immunogenicity often associated with subunit vaccines, making it a valuable component in immunological research and development. -
Immunoreactive Peptide
Muramyl dipeptide (MDP) is a synthetic immunoreactive peptide that targets NLRP1 and plays a significant role in bone formation. It induces osteoblast differentiation by up-regulating Runx2 gene expression via MAPK signaling pathways. Muramyl dipeptide is widely utilized in research focused on bone metabolism and immunological responses. -
ROS/NLRP3 Inflammasome Activator
Trimethylamine N-oxide is a gut microbiome-derived metabolite that primarily activates the ROS/NLRP3 inflammasome, leading to inflammatory responses. Its biological activity extends to promoting fibroblast-myofibroblast differentiation and inducing cardiac fibrosis through the TGF-β/smad2 signaling pathway. These properties make Trimethylamine N-oxide a valuable reagent for research into inflammation, fibrosis, and the interplay between dietary components and immune responses. -
NLRP3 Agonist
BMS-986299 is a first-in-class NLRP3 inflammasome agonist that exhibits potent activation with an EC50 of 1.28 μM. This compound is valuable for research exploring the role of NLRP3 in inflammatory processes and immune responses. Its ability to selectively stimulate the NLRP3 pathway makes it an important tool for studies related to autoinflammatory diseases and the development of novel immunotherapeutic strategies. -
NLRP3/AIM2 Inhibitor
NLRP3/AIM2-IN-3 is a selective inhibitor targeting the NLRP3 and AIM2 inflammasomes. This compound exhibits potent inhibitory activity against pyroptosis in THP-1 macrophages induced by LPS and nigericin, demonstrating an IC50 value of 0.077 ± 0.008 μM. NLRP3/AIM2-IN-3 disrupts the interactions between NLRP3 or AIM2 and the adaptor protein ASC, thereby preventing ASC oligomerization and subsequent inflammasome activation. This reagent is suitable for studies investigating inflammasome-mediated processes and pyroptotic cell death. -
NLRP3 Activator
QS-21-Api is a potent NLRP3 activator that functions as an immunostimulatory saponin, enhancing vaccine efficacy as an adjuvant. It stimulates both Th2 humoral and Th1 cell-mediated immune responses by acting on antigen presenting cells (APCs) and T cells. Through the activation of the NLRP3 inflammasome, QS-21-Api prompts the release of caspase-1 dependent cytokines, including IL-1β and IL-18, making it a valuable tool for research in immunology and vaccine development. -
NLRP1/3 Inhibitor
ADS032 is a sulfonylurea compound that functions as an inhibitor of the NLRP1 and NLRP3 inflammasomes. This compound effectively reduces the secretion of pro-inflammatory cytokines and inhibits the oligomerization of ASC, thereby exhibiting anti-inflammatory properties. ADS032 can be utilized in various research applications related to inflammatory diseases, making it a valuable tool for studying inflammasome-mediated pathways. -
Endogenous Metabolite
Desmosterol is a cholesterol precursor involved in the Bloch pathway of cholesterol biosynthesis. As an endogenous metabolite, it plays a critical role in the study of cholesterol metabolism. Desmosterol functions as a liver X receptor (LXR) activator and SREBP inhibitor, which can mitigate macrophage inflammasome activation, thereby reducing vascular inflammation and the risk of atherosclerosis. Furthermore, lower levels of Desmosterol can lead to increased production of mitochondrial reactive oxygen species (ROS) in macrophages and activate the NLRP3 inflammasome through pyrin domain mechanisms. This compound is valuable for research focused on inflammation, metabolic processes, and cardiovascular diseases. -
ROS/NLRP3 Inflammasome Activator
Trimethylamine N-oxide dihydrate is an activator of the ROS/NLRP3 inflammasome, functioning as a gut microbe-derived metabolite of dietary choline and other trimethylamine-rich nutrients. This compound promotes inflammatory responses and plays a role in the differentiation of fibroblasts to myofibroblasts, thereby contributing to cardiac fibrosis through the activation of the TGF-β/smad2 signaling pathway. Its properties make it valuable in studies focused on inflammation and fibrosis mechanisms in various biological contexts. -
Stable Isotope
Trimethylamine N-oxide-d9 is a deuterium-labeled form of Trimethylamine N-oxide, a gut microbiome-dependent metabolite derived from dietary choline and trimethylamine-rich nutrients. This compound has been shown to induce inflammation through the activation of the ROS/NLRP3 inflammasome. Additionally, Trimethylamine N-oxide is involved in accelerating fibroblast-to-myofibroblast differentiation, promoting cardiac fibrosis via the TGF-β/smad2 signaling pathway. It is a valuable reagent for research on metabolic disorders and cardiovascular diseases. -
NLRX1 Activator
Amelenodor is an NLRX1 activator that induces immunometabolic changes by selectively targeting the NLRX1 pathway. This compound demonstrates potential in reducing inflammation and modulating immune responses in inflammatory bowel diseases. Research applications include studies on Crohn's disease and ulcerative colitis, making it a valuable tool for advancing understanding of these conditions. -
NLRP3 Inhibitor
Selnoflast (RO7486967) is a highly selective and reversible small molecule inhibitor of the NLRP3 inflammasome. It effectively inhibits the release of IL-1β in response to NLRP3 activation in human monocyte-derived macrophages associated with Alzheimer's disease. Selnoflast is a valuable reagent for research into Alzheimer's disease and systemic inflammatory conditions, including ulcerative colitis and chronic obstructive pulmonary disease. -
AQP9 Inhibitor
RG100204 is a selective inhibitor of the aquaporin 9 (AQP9), targeting its channel function to obstruct the transmembrane transport of water, glycerol, and hydrogen peroxide (H2O2). This compound exhibits significant anti-inflammatory activity by reducing the activation of the NLRP3 inflammasome and the p38 MAPK signaling pathways, leading to decreased inflammation and pyroptosis. In preclinical studies, RG100204 has demonstrated the ability to mitigate multi-organ dysfunction in mouse models of sepsis and has shown potential glucose-regulating effects in diabetic db/db mice. -
NLRP3 Inhibitor
Ruvonoflast is a selective and orally active inhibitor of the NLRP3 inflammasome, effectively penetrating the central nervous system. With an IC50 of 0.32 nM, it inhibits IL-1β release in human peripheral blood mononuclear cells. Upon intracellular conversion to its active carboxylic acid form, Ruvonoflast demonstrates the ability to reverse obesity, systemic inflammation, and astrogliosis in mouse models of diet-induced obesity. This compound holds promise for research into neurodegenerative diseases such as Alzheimer's, Parkinson's, multiple sclerosis, and amyotrophic lateral sclerosis. -
NLRP3 Inflammasome Inhibitor
NP3-253 is a potent NLRP3 inflammasome inhibitor that exhibits oral bioavailability and can penetrate the blood-brain barrier. By acting as a molecular glue, NP3-253 stabilizes the NLRP3 protein in an inactive state, thereby effectively reducing the production of pro-inflammatory cytokines, including IL-1β and IL-18. This compound is valuable for studying inflammatory processes and neurological disorders, such as peritonitis, providing insights into therapeutic strategies for these conditions. -
NLRP3 Inhibitor
AZD4144 is a selective NLRP3 inhibitor with an effective concentration (EC50) of 0.082 μM. This compound significantly reduces the release of IL-1β associated with NLRP3 overactivation, demonstrating pronounced anti-inflammatory properties. With minimal impact on hERG and low cardiotoxicity, AZD4144 serves as a valuable tool for investigating diseases linked to NLRP3 inflammasome activation. -
NLRP3 Inflammasome Inhibitor
(±)11(12)-EET functions as an inhibitor of the NLRP3 inflammasome, playing a significant role in modulating inflammatory processes. This compound demonstrates potential anti-inflammatory, angiogenic, and cardioprotective properties, making it valuable for research aimed at understanding and treating inflammatory diseases and cardiovascular conditions. Its use in preclinical studies can provide insights into the mechanisms underlying these biological activities. -
KCNK13 Inhibitor
CVN293 is a selective inhibitor of the potassium ion channel KCNK13, demonstrating IC50 values of 41 nM and 28 nM for human and mouse KCNK13, respectively. This compound effectively suppresses the NLRP3 inflammasome-mediated production of the proinflammatory cytokine IL-1β in microglial cells. CVN293's brain permeability and targeted action make it a valuable tool for researching neuroinflammatory processes and potential therapeutic interventions.
