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-N6612
    D-Glucuronic acid
    		Agonist
    D-Glucuronic acid is a major component of many anti-inflammatory proteoglycans, which can promote embryonic development and inhibit cell aggregation. After being metabolized into ethyl glucuronide (HY-113093), D-Glucuronic acid activates Toll-like receptor 4 (TLR4), causing pain. D-Glucuronic acid and its derivative glucurono-lactone can serve as liver detoxifiers for human health prevention, and its derivatives also possess anti-tumor activity.
    D-Glucuronic acid
  • HY-134816
    D-Glucan
    		Activator
    D-Glucan is an orally effective Dectin-1 receptor immune activator with antioxidant properties (reducing TNF-α). D-Glucan activates macrophages and neutrophils to scavenge free radicals, inhibit oxidative stress and inflammatory responses, and improve insulin sensitivity. D-Glucan promotes glycolysis by enhancing the activity of the antioxidant enzyme glutathione, inhibiting gluconeogenesis and activating GK. D-Glucan can be used in the research of liver damage protection (antagonizing Acetaminophen (HY-66005) toxicity), radiation protection (synergistic with vitamin E) and diabetes (improving glucose metabolism).
    D-Glucan
  • HY-P1439A
    RS 09 TFA
    		Agonist 99.81%
    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-P1439
    RS 09
    		Agonist 99.88%
    RS 09 is an LPS (HY-D1056) peptide mimic and TLR4 agonist. RS 09 can bind to TLR-4 and activate NF-κB. RS 09 can function as an adjuvant in vivo, enhancing the antigen-specific immune response.
    RS 09
  • HY-D1056B3
    Lipopolysaccharides, from Klebsiella pneumoniae
    		Activator
    Lipopolysaccharides, from Klebsiella pneumoniae (LPS, from bacterial (Klebsiella pneumoniae)) are lipopolysaccharide endotoxins and TLR4 activators derived from Klebsiella pneumoniae, and are classified as S-type LPS. Lipopolysaccharides, from Klebsiella pneumoniae exhibit a typical three-part structure: O-antigen, core oligosaccharide, and lipid A. Lipopolysaccharides, from Klebsiella pneumoniae may participate in bacterial immune evasion by inhibiting complement-mediated killing and suppressing the host's secretion of antimicrobial peptides, thereby allowing the bacteria to escape immune defenses. Lipopolysaccharides, from Klebsiella pneumoniae possess high viscosity and resistance to serum-mediated killing, which may lead to sepsis. Lipopolysaccharides, from Klebsiella pneumoniae can be used to construct animal models of sepsis.
    Lipopolysaccharides, from Klebsiella pneumoniae
  • HY-117066
    CL075
    		Agonist 99.25%
    CL075 (3M002) is a selective TLR8 agonist with immunomodulating properties. CL075 triggers a MyD88-dependent signaling pathway to elicit production of inflammatory cytokines and type I interferons (IFNs) via activation of NF-κB and IRF7, respectively.
    CL075
  • HY-145917
    SARM1-IN-2
    		Inhibitor 99.34%
    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-B0892
    Benzyl alcohol
    		Activator 99.96%
    Benzyl alcohol is an aromatic alcohol, a colorless liquid with a mild aromatic odor. Benzyl alcohol is an inhibitor of P450 enzyme. Benzyl alcohol mediated Toll-Like Receptor 4 to reduce the inflammatory response of liver injury in mice.
    Benzyl alcohol
  • HY-150726
    ODN 1668
    		Agonist 98.79%
    ODN 1668, a class B CpG ODN (oligodeoxynucleotide), is a TLR-9 agonist. ODN 1668 has strong immune regulatory properties, can enhance the level of antibody IgG2 subtype, promote the immune response of T cells and B cells, and can be used in the study of vaccine adjuvants. In addition, CpG ODN 1668 induces an antimicrobial immune response via a CaTLR9 dependent pathway in groupers. Sequence: 5'-tccatgacgttcctgatgct-3’.
    ODN 1668
  • HY-125171
    IAXO-102
    		Antagonist ≥98.0%
    IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. IAXO-102 inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein. IAXO-102 also prevents experimental abdominal aortic aneurysm development.
    IAXO-102
  • HY-160229
    ssRNA40 sodium
    		Activator
    ssRNA40 (sodium) is a 20-mer phosphothioate protected single-stranded RNA oligonucleotide. ssRNA40 is a uridine-rich ssRNA derived from the HIV-1 long terminal repeat on activation of NK cells via TLR7/8[1][2].
    ssRNA40 sodium
  • HY-14806B
    Teneligliptin hydrobromide hydrate
    		Inhibitor 99.87%
    Teneligliptin (MP-513) hydrobromide hydrate is an orally active and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50s: 0.37 and 0.29 nM for the human and rat DPP-4, respectively). Teneligliptin hydrobromide hydrate improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus.
    Teneligliptin hydrobromide hydrate
  • HY-17367A
    Atazanavir sulfate
    		Inhibitor 99.94%
    Atazanavir (BMS-232632) sulfate is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir sulfate inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.
    Atazanavir sulfate
  • HY-N0774
    Isofraxidin
    		Inhibitor 99.00%
    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-103698
    TLR7/8 agonist 1
    		Agonist
    TLR7/8 agonist 1 is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.
    TLR7/8 agonist 1
  • HY-150738
    ODN 2088
    		Antagonist
    ODN 2088 is a potent TLR3, TLR7 and TLR9 inhibitor. ODN 2088 shows no cytotoxic. ODN 2088 inhibits the release of IFN-α and IL-6.
    ODN 2088
  • HY-103483
    MD2-IN-1
    		Inhibitor 99.89%
    MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD of 189 μM for the recombinant human MD2 (rhMD2).
    MD2-IN-1
  • HY-150738C
    ODN 2088 sodium
    		Antagonist
    ODN 2088 sodium is a potent TLR3, TLR7 and TLR9 inhibitor. ODN 2088 sodium shows no cytotoxic. ODN 2088 inhibits the release of IFN-α and IL-6.
    ODN 2088 sodium
  • HY-B0730
    Pamidronate disodium pentahydrate
    		Antagonist ≥98.0%
    Pamidronate disodium pentahydrate, the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronate disodium pentahydrate significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of osteoprotegerin 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, Pamidronate disodium pentahydrate can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma.
    Pamidronate disodium pentahydrate
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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