2. Signaling Pathways
  3. Immunology/Inflammation
  4. Toll-like Receptor (TLR)

Toll-like Receptor (TLR)

Toll-like Receptor (TLR)

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Toll-like receptors (TLRs) are a class of proteins that play a key role in the innate immune system. They are single, membrane-spanning, non-catalytic receptors usually expressed in sentinel cells such as macrophages and dendritic cells, that recognize structurally conserved molecules derived from microbes. Once these microbes have breached physical barriers such as the skin or intestinal tract mucosa, they are recognized by TLRs, which activate immune cell responses. The TLRs include TLR1, TLR2, TLR3, TLR4, TLR5, TLR6, TLR7, TLR8, TLR9, TLR10, TLR11, TLR12, and TLR13. Toll-Like Receptors (TLRs) play a critical role in the early innate immune response to invading pathogens by sensing microorganism and are involved in sensing endogenous danger signals. TLRs are evolutionarily conserved receptors are homologues of the Drosophila Toll protein, discovered to be important for defense against microbial infection. TLRs recognize highly conserved structural motifs known as pathogen-associated microbial patterns (PAMPs), which are exclusively expressed by microbial pathogens.

Toll-like Receptor (TLR) Isoform Specific Products:

Toll-like Receptor (TLR) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-103698
    TLR7/8 agonist 1
    		Agonist 98.42%
    TLR7/8 agonist 1 is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.
    TLR7/8 agonist 1
  • HY-150748A
    ODN D-SL01 sodium
    ODN D-SL01 sodium, a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. ODN D-SL01 sodium has strong immunostimulatory activity in a variety of vertebrate species and has anticancer activity. ODN D-SL01 sequence: 5'- T-C-G-C-G-A-C-G-T-T-C-G-C-C-C-G-A-C-G-T-T-C-G-G-T-A-3'.
    ODN D-SL01 sodium
  • HY-P1181A
    Pam2CSK4 TFA
    		Agonist 99.46%
    Pam2CSK4 TFA is a TLR2 agonist. Pam2CSK4 TFA induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 TFA activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 TFA expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 TFA acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 TFA can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis.
    Pam2CSK4 TFA
  • HY-17589B
    Chloroquine dihydrochloride
    		Inhibitor 99.61%
    Chloroquine dihydrochloride is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine dihydrochloride is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine dihydrochloride is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
    Chloroquine dihydrochloride
  • HY-N0774
    Isofraxidin
    		Inhibitor 99.94%
    Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells. Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation.
    Isofraxidin
  • HY-N7088
    Raffinose
    		Inhibitor 98.0%
    Raffinose (Melitose) regulates intestinal flora, inhibits TLR4-MyD88-NF-κB signaling pathway, and activates Nrf2 signaling pathway. Raffinose exhibits anti-inflammatory, antioxidant, and immunomodulatory activities. Raffinose is orally active.
    Raffinose
  • HY-112667
    CU-CPT-9a
    		Antagonist 99.74%
    CU-CPT-9a is a specific TLR8 antagonist, with an IC50 of 0.5 nM.
    CU-CPT-9a
  • HY-P99008
    Atibuclimab
    		Inhibitor ≥99.0%
    Atibuclimab (IC14), is a chimeric monoclonal antibody directed against CD14 and is composed of murine variable and human IgG4 Fc regions. Atibuclimab attenuates Lipopolysaccharides (HY-D1056) (LPS)-induced symptoms and strongly inhibits LPS-induced proinflammatory cytokine release, while only delaying the release of the anti-inflammatory cytokines soluble TNF receptor type I and IL-1 receptor antagonist. Atibuclimab can be used for the research of amyotrophic lateral sclerosis, sepsis, community-acquired pneumonia, or acute lung injury.
    Atibuclimab
  • HY-139323
    TLR7/8-IN-1
    		Inhibitor 99.92%
    TLR7/8-IN-1 is a crystalline from of a TLR7/TLR8 inhibitor extracted from patent WO2019220390, compound 2b. TLR7/8-IN-1 can be used for the research of autoimmune disease.
    TLR7/8-IN-1
  • HY-N7700A
    Guluronic acid sodium
    		Inhibitor 98.0%
    Guluronic acid (G2013) sodium is an orally active oxidative stress regulator and anti-inflammatory agent that exerts pharmacological effects by down-regulating various pro-inflammatory and oxidative stress-related genes (such as TLR4, NF-κB, iNOS, etc.) and inhibiting the activities of COX-2, MMPs and VEGF. Low-dose Guluronic acid sodium up-regulates the expression of immunoregulatory genes SHIP1 and SOCS1, thereby effectively inhibiting cancer-related inflammation, tumor angiogenesis, cell adhesion and metastasis, while reducing the accumulation of immunosuppressive cells. Guluronic acid sodium significantly prolongs the survival time of tumor-bearing hosts within a concentration range without direct cytotoxicity, demonstrating favorable safety. Guluronic acid sodium has involved in the research of multiple sclerosis, ankylosing spondylitis, breast cancer and other inflammatory diseases.
    Guluronic acid sodium
  • HY-D1056A2
    Lipopolysaccharides, from E. coli O127:B8
    		Activator
    Lipopolysaccharides, from E. coli O127:B8 (LPS, from Escherichia coli (O127:B8)) are endotoxins and TLR4 activators extracted from Escherichia coli (E. coli O127:B8) and are classified as S (smooth) type LPS. Lipopolysaccharides, from E. coli O127:B8 possess the typical three-part structure: O-antigen, R3-type core oligosaccharide, and lipid A. Lipopolysaccharides, from E. coli O127:B8 activate TLR-4 in immune cells, can induce inflammatory responses and ileal contractility, and can be used to construct intestinal inflammation models.
    It is recommended to prepare a solution with concentration ≥2 mg/mL. Vortex thoroughly for more than 10 minutes. Due to the adsorption characteristics of LPS, silanized container or low adsorption centrifuge tubes should be used for aliquoting and storage, and mix thoroughly before use.
    Lipopolysaccharides, from E. coli O127:B8
  • HY-P1439A
    RS 09 TFA
    		Agonist 99.87%
    RS 09 TFA is an LPS (HY-D1056) peptide mimic and TLR4 agonist. RS 09 TFA can bind to TLR-4 and activate NF-κB. RS 09 TFA can function as an adjuvant in vivo, enhancing the antigen-specific immune response.
    RS 09 TFA
  • HY-145917
    SARM1-IN-2
    		Inhibitor 99.97%
    SARM1-IN-2 (Example 82) is a SARM1 inhibitor (IC50 <1 μM) that inhibits axon regeneration. Axon regeneration refers to the process by which neuronal axons attempt to restore their structure and function after axonal degeneration. SARM1-IN-2 inhibits axon regeneration by reducing or inhibiting the binding of SARM1 to NAD+. SARM1-IN-2 can be used to study axonal degeneration.
    SARM1-IN-2
  • HY-D1056A4
    Lipopolysaccharides, from E. coli O128:B12
    		Activator
    Lipopolysaccharides, from E. coli O128:B12 (LPS, from Escherichia coli (O128:B12)) are endotoxins and TLR4 activators extracted from Escherichia coli (E. coli O128:B12) and are classified as S (smooth) type LPS. Lipopolysaccharides, from E. coli O128:B12 possess the typical three-part structure: O-antigen, R3-type core oligosaccharide, and lipid A. Lipopolysaccharides, from E. coli O128:B12 activate TLR-4 in immune cells, can be used to construct animal models of neonatal brain inflammation, and may influence preterm birth in neonates.
    It is recommended to prepare a solution with concentration ≥2 mg/mL. Vortex thoroughly for more than 10 minutes. Due to the adsorption characteristics of LPS, silanized container or low adsorption centrifuge tubes should be used for aliquoting and storage, and mix thoroughly before use.
    Lipopolysaccharides, from E. coli O128:B12
  • HY-B0012
    Pamidronic acid
    		Inhibitor 99.05%
    Pamidronic acid, the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronic acid significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of OPG in cartilage and subchondral bone, and inhibiting the expression of RANKL and MMP-9 in both tissues, as well as TLR-4 in cartilage, thereby alleviating cartilage degeneration. Additionally, Pamidronic acid can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma.
    Pamidronic acid
  • HY-P99555
    Tomaralimab
    		Inhibitor 99.42%
    Tomaralimab (OPN-305) is a humanized anti-TLR2 IgG4 monoclonal antibody. Tomaralimab inhibits TLR2, MyD88, NLRP3, and reduces pro-inflammatory cytokine (IL-1β, IL-6, IL-8) production. Tomaralimab reduces tau pathology. Tomaralimab improves cognition, atopic dermatitis. Tomaralimab has anticancer effects on pancreatic ductal adenocarcinoma. Tomaralimab is being studied in myelodysplastic syndrome (MDS), atopic dermatitis, pancreatic ductal adenocarcinoma, Alzheimer's disease, and myocardial ischemia/reperfusion injury.
    Tomaralimab
  • HY-17589R
    Chloroquine phosphate (Standard)
    		Inhibitor
    Chloroquine (phosphate) (Standard) is the analytical standard of Chloroquine (phosphate). This product is intended for research and analytical applications. Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
    Chloroquine phosphate (Standard)
  • HY-148980A
    Polyinosinic acid sodium
    Polyinosinic acid sodium is the sodium form of Polyinosinic acid (HY-148980). Polyinosinic acid is a single stranded homonucleic acid, which is a Toll-like Receptor 3 (TLR3) ligand. Polyinosinic acid enhances cellular immune response through TLR3 and TRIF. Polyinosinic acid has potential applications in immune regulation.
    Polyinosinic acid sodium
  • HY-106950
    Fosfructose
    		98.0%
    Fosfructose is an orally active cyclooxygenase-2 inhibitor and Toll-like receptor 4 modulator. Fosfructose reduces the expression of cyclooxygenase-2, thereby decreasing prostaglandin production. By inhibiting the Toll-like receptor 4 signaling pathway, Fosfructose downregulates LPS-induced adhesion molecule expression. Fosfructose is applicable to research related to ischemic stroke, epilepsy, sepsis, myocardial injury, osteoporosis, and ultraviolet B-induced skin damage.
    Fosfructose
  • HY-U00435
    Neoseptin 3
    		Agonist 99.21%
    Neoseptin 3 is a Toll-like receptor 4/myeloid differentiation factor 2 (mTLR4/MD-2) agonist with an EC50 of 18.5 μM.
    Neoseptin 3
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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