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-153073
    TLR7 agonist 8
    Agonist
    TLR7 agonist 8 is a TLR7 agonist with an EC50 of 0.12 nM for TLR7 and an EC50 of 0.76 nM for IL-6 induction. TLR7 agonist 8 can be used for research on diseases such as fibrosis, inflammatory diseases, cancer, or pathogen infections.
    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-183079
    ENDO12
    Inhibitor
    ENDO12 is an inhibitor of the Munc13-4-STX7 protein complex, with a Kd value of 2.7 µM for STX7. ENDO12 blocks the interaction of Munc13-4-STX7. ENDO12 inhibits endolysosomal flux, endolysosomal cargo degradation, the extracellular signal-regulated kinase signaling pathway in neutrophils, the IFN regulatory factor signaling pathway in plasmacytoid dendritic cells, and the responses of primary dendritic cells to TLR3, TLR7, and TLR9. ENDO12 alleviates CpG-induced systemic inflammation by reducing the levels of myeloperoxidase, IL-6 and IFNγ. ENDO12 does not interfere with the host's antiviral response to lymphocytic choriomeningitis virus infection.\nENDO12 can be used in studies related to systemic inflammation.
    ENDO12
  • HY-20457G
    TL8-506 (GMP)
    Agonist
    TL8-506 (GMP) is TL8-506 (HY-20457) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 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 (GMP)
  • 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-N19801
    N-Palmitoyl-D-glucosamine
    Antagonist
    N-Palmitoyl-D-glucosamine is an orally active TLR4 antagonist. N-Palmitoyl-D-glucosamine stably binds MD-2 with, preventing LPS-induced NF-κB signaling, decreases pro-inflammatory cytokines (IL-1β, TNF-α, and IL-6), increases anti-inflammatory IL-10 and IL-1rα, and normalizes miR-20a-5p, miR-106a-5p, and miR-27a-3p levels. N-Palmitoyl-D-glucosamine decreases allodynia and prevents myelino-axonal degeneration of peripheral nerves. N-Palmitoyl-D-glucosamine can be used for the researches of keratitis and peripheral neuropathy.
    N-Palmitoyl-D-glucosamine
  • HY-160040A
    Cobitolimod sodium
    Agonist
    Cobitolimod sodium is a DNA oligonucleotide agonist of TLR-9 with anti-inflammatory activity. Cobitolimod sodium inhibits Th17 cells and induces anti-inflammatory FoxP3 and IL-10 expression, inhibiting the IL-17 signaling pathway.
    Cobitolimod sodium
  • HY-176755
    CCL-34
    Activator
    CCL-34 is a Toll-like receptor 4 (TLR4) activator. CCL-34 significantly induced dendritic cell (DC) CD83 expression and IL-12p70 production in a dose-dependent manner, thereby inducing DC maturation. CCL-34 enhanced the allostimulatory activity of DC on naive CD4+CD45+RA+ T cell proliferation and IFN-γ secretion. CCL-34 further induced antigen presentation ability in mice inoculated with doxorubicin-treated colorectal cancer cells. CCL-34 can be used in studies of immune stimulation.
    CCL-34
  • HY-153544
    TLR7/8 agonist 9
    Inhibitor
    TLR7/8 agonist 9 (Compound 25a) is a TLR7/8 agonist, with EC50s of 40 nM and 23 nM for hTLR7/8. TLR7/8 agonist 9 has anti-tumor activity and improves the antitumor activity of PD-1/PD-L1 blockade. TLR7/8 agonist 9 can be used for research of cancer immunotherapy.
    TLR7/8 agonist 9
  • HY-B0380S2
    Trimebutine-d3 hydrochloride
    Inhibitor
    Trimebutine-d3 hydrochloride is deuterium labeled Trimebutine hydrochloride. Trimebutine hydrochloride is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine hydrochloride inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine hydrochloride also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine hydrochloride also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine hydrochloride also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
    Trimebutine-d<sub>3</sub> hydrochloride
  • HY-N6949R
    Juglone (Standard)
    Inhibitor
    Juglone (Standard) is the analytical standard of Juglone. This product is intended for research and analytical applications. Juglone (5-hydroxy-1,4-naphthalenedione) is a yellow dye that can be extracted from Juglans regia. Juglone induces apoptosis through the mitochondrial pathway. Juglone has antibacterial and antitumor activity .
    Juglone (Standard)
  • HY-161026
    JM-9
    Inhibitor
    JM-9 is a inhibitor of MD2. JM-9 suppresses high glucose and palmitic acid -induced inflammation in MPMs. JM-9 improves diabetic kidney disease by inhibiting MD2-mediated inflammation.
    JM-9
  • HY-177648A
    Nelitolimod sodium
    Agonist
    Nelitolimod sodium, a CpG oligonucleotide, is a TLR9 agonist.
    Nelitolimod sodium
  • HY-P11442
    Lytx-Pa2a
    Inhibitor
    Lytx-Pa2a (Lycotoxin-Pa2a) is a peptide inhibitor against bacterial membranes and TLR4 receptor. Lytx-Pa2a exerts antimicrobial effects via non-competitive disruption of outer/cytoplasmic membranes and suppression of LPS-induced TLR4/NF-κB signaling. Lytx-Pa2a is promising for research of bacterial infection and inflammation-related disease (e.g., sepsis).
    Lytx-Pa2a
  • HY-182369
    VA06
    Inhibitor
    VA06 is a derivative of QS-21 (HY-101092A) that retains potent adjuvant activity while significantly reducing toxicity. VA06 self-assembles into flexible worm-like micelles with continuously elongated nanostructures and enhanced drug-loading encapsulation capacity. VA06 induces antigen-specific antibody production, enhances the secretion of TNF-α, IFN-γ and IL-2 in CD4+ and CD8+ T cells, and promotes the expression of immune-related and antiviral-related genes in mature dendritic cells. VA06 does not require liposome formulation, which simplifies production and storage processes. VA06 can be used in the research of varicella-zoster virus infection and Mycobacterium tuberculosis infection.
    VA06
  • HY-P990520
    Anti-TLR7 Antibody
    Inhibitor ≥99.0%
    Anti-TLR7 Antibody is a CHO-expressed human antibody that targets TLR7. Anti-TLR7 Antibody contains huIgG1 heavy chain and huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for Anti-TLR7 Antibody can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-TLR7 Antibody
  • HY-159744
    Liposomal adjuvant (M103)
    Activator
    Liposomal adjuvant (M103) is mainly composed of phospholipids and prepared with highly purified immunostimulatory substances (polysaccharides), with a pH value of 6.2-6.8. This adjuvant is safe, non-toxic, and metabolizable. It can induce cellular and humoral immunity, has a sustained-release effect, and can prolong the residence time of antigens in the body. This adjuvant is suitable for various veterinary vaccines, including inactivated vaccines and genetically engineered subunit vaccines. It is recommended for use in rabies, porcine circovirus, , foot-and-mouth disease (FMD), and blue ear disease, etc.
    Liposomal adjuvant (M103)
  • HY-162116
    TLR7 agonist 18
    Agonist
    TLR7 agonist 18 (Compound 21a) is a selective Toll-like receptor 7 (TLR7) agonist with an EC50 of 7.8 μM. TLR7 agonist 18 is not cytotoxic to hTLR7 cotransfected HEK293 cell lines and can induce the secretion of several cytokines, including IL-1β, IL-12p70, IL-8, and TNF-α. TLR7 agonist 18 can be used in vaccine, asthma, allergy and anti-cancer research.
    TLR7 agonist 18
  • HY-177623A
    CpG-ODN c41 sodium
    Agonist
    CpG-ODN c41 sodium, an oligonucleotide, is an antagonist of TLR9.
    CpG-ODN c41 sodium
  • HY-145254
    Tri(TLR4-IN-C34-PEG2-amide-PEG1)-amide-C3-COOH
    Inhibitor
    Tri(TLR4-IN-C34-PEG2-amide-PEG1)-amide-C3-COOH is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.
    Tri(TLR4-IN-C34-PEG2-amide-PEG1)-amide-C3-COOH
Cat. No. Product Name / Synonyms Species Source
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