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-169017
    MTT5
    Agonist
    MTT5 is a toll-like receptor 7 (TLR7) agonist. MTT5 can couple with Deruxtecan (HY-13631E) and exert anti-tumor activity in HER2 positive solid tumors through tumor cell killing and immune activation.
    MTT5
  • HY-161726
    TLR7 agonist 23
    Agonist
    TLR7 agonist 23 (compound 12b) is a potent Toll Like Receptor-7 (TLR7) agonist with a EC50 of 0.15 uM. TLR7 agonist 23 can be used in the study of immunological diseases.
    TLR7 agonist 23
  • HY-N7697C
    Chitohexaose hexahydrochloride
    Chitohexaose hexahydrochloride is a chitosan oligosaccharide with anti-inflammatory effect. Chitohexaose hexahydrochloride binds to the active sites of TLR4 and inhibits LPS induced inflammation.
    Chitohexaose hexahydrochloride
  • HY-150725A
    Biotin-labeled ODN 1585 sodium
    Biotin-labeled ODN 1585 (sodium) is a potent inducer of IFN and TNFα production. Biotin-labeled ODN 1585 (sodium) can be used to evaluate CpG ODN cellular uptake and localization using a biotin detection system and light microscopy.
    Biotin-labeled ODN 1585 sodium
  • HY-153841A
    ODN INH-1 sodium
    Inhibitor
    ODN INH-1 sodium is palindromic and a class R (‘restricted’) inhibitory ODN. ODN INH-1 sodium is a potent inhibitor of TLR9-induced B cells and macrophages
    ODN INH-1 sodium
  • HY-163998
    TLR4-IN-1
    TLR4-IN-1 (compound 3k) inhibits the cell viability of RAW264.7 with an IC50 of 1.02 μM. TLR4-IN-1 inhibits the release of cytokine TNF-α, IL-1β and IL-6, and exhibits anti-inflammatory efficacy in rats rheumatoid arthritis models.
    TLR4-IN-1
  • HY-114592
    M199
    Inhibitor
    M199 is a potent TLR3/TLR9 signaling inhibitor. M199 induces secretion of IL-6, IL-8 and TNFα in human PBMCs. M199 is used as a selective inducer of the immune response.
    M199
  • HY-14750
    Rabeximod
    Rabeximod (ROB-803), an anti-rheumatic compound, impairs the differentiation and function of human pro-inflammatory dendritic cells and macrophages via downregulating TLR2 and TLR4 stimulation. Rabeximod (ROB-803) is used for rheumatoid arthritis (RA) research.
    Rabeximod
  • HY-156177
    TLR7 agonist 16
    Agonist
    TLR7 agonist 16 (compound 16d) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 16 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations.
    TLR7 agonist 16
  • HY-159178
    m-AM-BBIQ
    Agonist
    m-AM-BBIQ (compound 10) is a dual TLR7 and TLR8 agonist, with EC50 values of 0.12 μM and 1.7 μM for hTLR7 and hTLR8, respectively.
    m-AM-BBIQ
  • HY-150216
    ODN 105871
    Inhibitor
    ODN 105871, a G-modified inhibitory oligonucleotide (INH-ODN), is a selective TLR7 inhibitor. ODN 105871 can be uesd for inflammatory immune responses research.
    ODN 105871
  • HY-162649
    TIC10g
    Inhibitor
    TIC10g is a dual inhibitor for toll-like receptor 7 and 9 (TLR7 and TLR9), which inhibits TLR7 and TLR9 mediated TNF-α release in mouse macrophages (IC50 is 14.5 μM and 6.5 μM) and human B lymphocytes (IC50 is 7.69 μM and 11.5 μM). TIC10g inhibits the activation of NF-κB and MAPK, and exhibits anti-inflammatory activity against systemic lupus erythematosus and rheumatoid arthritis .
    TIC10g
  • HY-156693
    MTvkPABC-P5
    Agonist
    MTvkPABC-P5d, a TLR7 agonist, is an immune stimulant. MTvkPABC-P5d can be used for synthesis of immune-stimulating antibody conjugates (ISACs).
    MTvkPABC-P5
  • HY-B0012B
    Pamidronic acid sodium
    Inhibitor
    Pamidronic acid sodium, the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronic acid sodium 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 sodium can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma.
    Pamidronic acid sodium
  • HY-17589S1
    Chloroquine-d4 phosphate
    Inhibitor
    Chloroquine-d4 (phosphate) is the deuterium labeled Chloroquine phosphate. 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)[1][2][3][4].
    Chloroquine-d<sub>4</sub> phosphate
  • HY-153073
    TLR7 agonist 8
    Agonist
    TLR7 agonist 8 (compound IIb-34) is an TLR7 agonist with an EC50 value of ~4 nM.
    TLR7 agonist 8
  • HY-156176
    TLR7 agonist 15
    Agonist
    TLR7 agonist 15 (compound 16b) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 15 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations.
    TLR7 agonist 15
  • HY-131262
    Hydroxychloroquine Impurity E
    99.83%
    Hydroxychloroquine Impurity E is the impurity of Hydroxychloroquine. Hydroxychloroquine is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro.
    Hydroxychloroquine Impurity E
  • HY-150212
    Tilsotolimod
    Inhibitor
    Tilsotolimod is a synthetic Toll-like receptor 9 (TLR9) agonist that has demonstrated antitumor activity in preclinical models.
    Tilsotolimod
  • HY-W782032
    3D-Monophosphoryl Lipid A-5
    Agonist
    3D-Monophosphoryl Lipid A-5 (3D-MPLA-5) is a TLR agonist that can be used as an adjuvant for vaccines to enhance their immunogenicity.
    3D-Monophosphoryl Lipid A-5
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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