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

Toll-like Receptor (TLR)

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N0217
    Benzoylaconine
    Inhibitor 99.92%
    Benzoylaconine (Benzoylaconitine) is an orally active monoester alkaloid found in the traditional Chinese medicine Aconitum carmichaelii. Benzoylaconine is an ACE2 agonist (EC50: 1.5 μM) with antihypertensive and anti-heart failure effects. Benzoylaconine inhibits TLR-induced MAPK and NF-κB pathways to exert anti-inflammatory effects. Benzoylaconine upregulates the protein levels of P-gp, MRP2, and has anti-tumor effects.
    Benzoylaconine
  • HY-14806B
    Teneligliptin hydrobromide hydrate
    Inhibitor 99.97%
    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-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-N0741A
    Leonurine hydrochloride
    99.43%
    Leonurine hydrochloride is an alkaloid isolated from Leonurus artemisia, with anti-oxidative and anti-inflammatory.
    Leonurine hydrochloride
  • HY-160229
    ssRNA40 sodium
    Activator 98.34%
    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-103697
    Gardiquimod
    99.91%
    Gardiquimod is an imidazoline TLR7/8 agonist. Gardiquimod inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 at concentrations below 10 μM.
    Gardiquimod
  • HY-17003
    Saquinavir mesylate
    Inhibitor 99.84%
    Saquinavir (Ro 31-8959) mesylate is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir mesylate also has anti-inflammatory activity and can induce apoptosis of human red blood cells.
    Saquinavir mesylate
  • HY-N0625A
    Alpinetin
    Inhibitor 99.51%
    Alpinetin is a flavonoid isolated from cardamom and possesses antitumor, antiinflammation, hepatoprotective, cardiovascular protective, lung protective, antibacterial, antiviral, neuroprotective properties. Alpinetin inhibits lipopolysaccharide (LPS)-induced inflammation, activates PPAR-γ, activates Nrf2, and inhibits TLR4 expression to protect LPS-induced renal injury.
    Alpinetin
  • 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-N1346
    Robinin
    Inhibitor 99.09%
    Robinin is a flavonoid that can be extracted from the leaves of purple cowpea, inhibiting TGF-β, TLR4/NF-κB and TLR2-PI3k-AKT signaling pathways. Robinin exerts anti-inflammatory and anti-tumor effects. The combination of Robinin and Methotrexate (HY-14519) reduces inflammation in experimental arthritis, Robinin can decrease the Doxorubicin (HY-15142A) induced cardiac toxicity effect.
    Robinin
  • HY-20457
    TL8-506
    Agonist
    TL8-506 is a specific TLR8 agonist with an EC50 of 30 nM. TL8-506 has immunomodulatory effects and can be used in the study of tuberculosis and cancer immunotherapy.
    TL8-506
  • HY-150738C
    ODN 2088 sodium
    Antagonist 98.82%
    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-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-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
  • 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-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-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-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-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-153808B
    Complete Freund's adjuvant (CFA, 1 mg/ml)
    Complete Freund's adjuvant (CFA, 1 mg/ml) is an immunoadjuvant emulsified with antigen that can enhance an animal's immune response to an antigen. Complete Freund's adjuvant (CFA, 1 mg/ml) is also an inducer of the Th1 immune response and a ligand of TLRs. Complete Freund's adjuvant (CFA, 1 mg/ml) contains heat-killed inactive tuberculosis bacilli and consists of a paraffin oil-in-water emulsion. Complete Freund's adjuvant (CFA, 1 mg/ml) stimulates a strong and durable immune response and can be used to induce rheumatoid arthritis in rats, and more.
    Complete Freund's adjuvant (CFA, 1 mg/ml)
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