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-D1056A2
    Lipopolysaccharides, from E. coli O127:B8
    Activator
    Lipopolysaccharides, from E. coli O127:B8 is a lipopolysaccharide endotoxin from E. coli O127:B8 and TLR-4 activator, Activates disease-associated molecular patterns (PAMPs) of the immune system and induces cell secretion of migratory bodies. Lipopolysaccharides, from E. coli O127:B8 consists of an antigen-specific O-chain, A core oligosaccharide, and lipid A. Lipopolysaccharides, from E. coli O127:B8 can induce changes in body temperature in rats and is dose and serotype specific. High dose of Lipopolysaccharides, from E. coli O127:B8 can cause a double change of body temperature in rats, that is, hypothermia followed by fever. In addition, Lipopolysaccharides, from E. coli O127:B8 can induce inflammation and inhibit reproduction, and can significantly increase the mitotic activity of mollusks.
    Lipopolysaccharides, from E. coli O127:B8
  • HY-150742
    ODN 2336
    Agonist
    ODN 2336 is a A-Class CpG ODN (oligodeoxynucleotides), is a potent TLR9 agonist. ODN 2336 induces the production of IFN-α. ODN 2336 up-regulates the expression of IP-10 mRNA and IL-18 mRNA. ODN 2336 can be used as adjuvant of vaccines.
    ODN 2336
  • HY-103639A
    M62812
    Inhibitor 99.86%
    M62812 is a toll-like receptor 4 (TLR4) signaling inhibitor. M62812 inhibits endothelial and leukocyte activation and prevents lethal septic shock in mice. M62812 can reduces LPS-induced coagulation and inflammatory responses. M62812 can be used for the research of sepsis.
    M62812
  • HY-110207
    SM-324405
    Agonist 98.52%
    SM-324405 is a TLR7 agonistic antedrug (EC50 = 50 nM), with pEC50 values of 7.3 and 6.6 for human TLR7 and Rat TLR7, respectively. SM-324405 is used for immunoresearch of allergic diseases. An antedrug is defined as a locally active compound that is designed to be rapidly metabolized to an inactive form upon entry into the circulation and prevents systemic toxicity by losing its agonistic activity in a plasmatic environment.
    SM-324405
  • HY-100176
    PF-4878691
    Agonist 99.89%
    PF-4878691 (3M-852A) is an orally active TLR7 agonist. PF-4878691 has the innate immune response activity, antiviral efficacy against HCV, and can be used for the research of cancer.
    PF-4878691
  • HY-148338
    TLR8 agonist 5
    Agonist
    TLR8 agonist 5 is a potent TLR8 agonist with an EC50 value of 20 nM for HEK-Blue hTLR8. TLR8 agonist 5 activates the immune response.
    TLR8 agonist 5
  • HY-128799A
    CL097 hydrochloride
    Agonist 99.90%
    CL097, a potent TLR7 and TLR8 agonist, induces pro-inflammatory cytokines in macrophages. CL097 induces NADPH oxidase priming, resulting in an increase of the fMLF-stimulated ROS production.
    CL097 hydrochloride
  • HY-P99555
    Tomaralimab
    Inhibitor
    Tomaralimab (OPN-305) is a humanised anti-TLR2 IgG4 monoclonal antibody. Tomaralimab has the potential for the research of Myelodysplastic Syndromes (MDS).
    Tomaralimab
  • HY-150750A
    ODN M362 sodium
    ODN M362 sodium, a class C oligodeoxynucleotide, is a TLR-9 agonist and can be used as a vaccine adjuvant. ODN M362 sodium induces cancer cell apoptosis.
    ODN M362 sodium
  • HY-111582
    BBIQ
    Agonist 99.85%
    BBIQ is a imidazoquinoline compound and a potent and selectively toll-like receptor 7 (TLR7) agonist with an EC50 of ?59.1?nM for human TLR7. BBIQ is a powerful vaccine adjuvant that enhances innate immune responses.
    BBIQ
  • HY-150748
    ODN D-SL01
    Agonist 99.94%
    ODN D-SL01, a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. ODN D-SL01 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
  • HY-W008634
    Bropirimine
    Agonist 99.92%
    Bropirimine is a synthetic agonist for toll-like receptor 7 (TLR7). Bropirimine inhibits differentiation of osteoclast precursor cells into osteoclasts via TLR7-mediated production of IFN-β. Bropirimine is an orally active immunomodulator that has demonstrated anticancer activity in transitional cell carcinoma in situ (CIS) in both the bladder and upper urinary tract.
    Bropirimine
  • HY-146195
    MAPK-IN-1
    Inhibitor
    MAPK-IN-1 (Compound 2) is a MAPK signaling pathway inhibitor. MAPK-IN-1 exhibits AChE inhibitory activity with an IC50 of 23.84 μM. MAPK-IN-1 shows anti-neuroinflammatory and neuroprotective activity and can be used for Alzheimer's disease research.
    MAPK-IN-1
  • HY-17589AS
    Chloroquine-d5
    Inhibitor ≥99.0%
    Chloroquine-d5 is deuterium labeled Chloroquine (HY-17589A). Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
    Chloroquine-d<sub>5</sub>
  • HY-111358
    TLR7 agonist 1
    Agonist 98.19%
    TLR7 agonist 1 is a potent, selective and oral TLR7 agonist with an IC50 of 90 nM.
    TLR7 agonist 1
  • HY-111269
    AZD8848
    Agonist 99.14%
    AZD8848 is a selective toll-like receptor 7 (TLR7) anteagent agonist which is developed for the research of asthma and allergic rhinitis.
    AZD8848
  • HY-144619
    TLR7/8 antagonist 2
    Antagonist 99.68%
    TLR7/8 antagonist 2 (Compound 15) is a potent and orally active agonist of TLR7/8 with IC50s of 4.9 and 0.6 nM, respectively. Inappropriate activation of TLR7 and TLR8 is linked to several autoimmune diseases, such as lupus erythematosus. TLR7/8 antagonist 2 has the potential for the research of autoimmune diseases.
    TLR7/8 antagonist 2
  • HY-150744A
    ODN 24888 sodium
    ODN 24888 sodium is an guanine-modified inhibitory oligonucleotides (INH-ODN), shows potent inhibition on TLR7/TLR9-mediated signaling. ODN 24888 sodium impairs IFN-α level and NF-κB activation, inhibits IL-6 release. ODN 24888 sodium involves in immune and inflammatory responses, can be used as a vaccine adjuvant.
    ODN 24888 sodium
  • HY-150745A
    ODN 24987 sodium
    ODN 24987 sodium is a Guanine-modified inhibitory oligonucleotides (ODN), targeting TLR9. ODN 24987 can inhibit IL-6 and IFN-α release. ODN 24987 sodium can be used for research immune disorders. ODN 24987 sequence: 5’-C-C-T-G-G-C-c7G-G-G-G-3’.
    ODN 24987 sodium
  • HY-145645
    Paridiprubart
    Inhibitor
    Paridiprubart (NI-0101) is a humanised anti-TLR4 monoclonal antibody. Paridiprubart has the potential for the research of rheumatoid arthritis.
    Paridiprubart
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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