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-161630
    TLR8 agonist 8
    		Agonist
    TLR8 agonist 8 (Compound II-72) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 8 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 8 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 89%.
    TLR8 agonist 8
  • HY-D1056B2
    Lipopolysaccharides, from Proteus mirabilis
    Lipopolysaccharides, from Proteus mirabilis are lipopolysaccharide endotoxins and TLR-4 activators derived from Proteus mirabilis, classified as S-type LPS, which can activate pathogen-associated molecular patterns (PAMP) of the immune system and induce cellular secretion of migrasomes. Lipopolysaccharides, from Proteus mirabilis exhibit a typical three-part structure: O-antigen, core oligosaccharide, and lipid A. Proteus mirabilis is a major pathogen causing urinary tract infections and may also contribute to rheumatoid arthritis. Lipopolysaccharides, from Proteus mirabilis also exhibit potential anti-tumor effects, demonstrating in vivo inhibitory activity against solid tumors such as meningosarcoma and Walker carcinosarcoma.
    It is recommended to prepare a stock solution of ≥2 mg/mL and ensure that it is fully mixed and dissolved. Due to the adsorption characteristics of LPS, low adsorption centrifuge tubes should be used for aliquoting and storage.
    Lipopolysaccharides, from Proteus mirabilis
  • HY-153839A
    ODN 4084-F sodium
    		Inhibitor
    ODN 4084-F sodium is a class B (‘broadly-active’) inhibitory ODN. ODN 4084-F sodium is potent inhibitor of TLR9-induced B cells and macrophages.
    ODN 4084-F sodium
  • HY-17007S
    Saquinavir-d9
    		Inhibitor
    Saquinavir-d9 (Ro 31-8959-d9) is the deuterium labeled Saquinavir (HY-17007). Saquinavir (Ro 31-8959) is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir also has anti-inflammatory activity and can induce apoptosis of human red blood cells.
    Saquinavir-d<sub>9</sub>
  • HY-145253
    Tri(TLR4-IN-C34-C2-amide-PEG1)-amide-C3-COOH
    		Inhibitor
    Tri(TLR4-IN-C34-C2-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-C2-amide-PEG1)-amide-C3-COOH
  • HY-P10208
    RKH
    		Antagonist
    PKH is a TLR4 antagonist. PKH is a novel tripeptide and can be isolated from Akkermansia muciniphila. RKH reduces sepsis-induced inflammatory cell activation and proinflammatory factor overproduction.
    RKH
  • HY-176487
    SARM1-IN-6
    SARM1-IN-6 (Compound 17a) is a brain-permeable SARM1 orthosteric inhibitor with IC50 of 14 nM for NAM and 74 nM for HEK cells.
    SARM1-IN-6
  • HY-139785A
    Cavrotolimod sodium
    		Inhibitor
    Cavrotolimod sodium is an immunostimulatory spherical nucleic acid (SNA) modified with type B CpG oligonucleotides designed to agonize TLR9 and elicit immune responses useful in oncology applications.
    Cavrotolimod sodium
  • HY-N4093R
    Astringin (Standard)
    		Inhibitor
    Astringin (trans-Astringin) (Standard) is the analytical standard of Astringin (HY-N4093). This product is intended for research and analytical applications. Astringin (trans-Astringin) is an orally active natural flavonoid compound. Astringin can inhibit the production of oxidative stress, inflammatory factors, etc. Astringin has multiple activities such as anti-oxidation, anti-inflammation, and anti-apoptosis. Astringin is also an inhibitor of ferroptosis. Astringin can be used in the research of diseases such as acute lung injury.
    Astringin (Standard)
  • HY-149650A
    TLR4 agonist-1 TEA
    		Agonist
    TLR4 agonist-1 (TEA) (compound 17a) is a potent agonist of Toll-like Receptor 4 (TLR4), and induces the generation of MIP-1β in RAW 264.7 and MM6 cells.
    TLR4 agonist-1 TEA
  • HY-W754114
    Nalmefene Sulfate-d3
    Nalmefene Sulfate-d3 is the deuterium labeled Nalmefene (HY-107744). Nalmefene is a BBB-penetrable opioid receptor modulator. Nalmefene is an antagonist of MOR and DOR, and a partial agonist of KOR. Nalmefene has anti-inflammatory and neuroprotective activities. Nalmefene can be used in the research of reducing alcohol-dependent disorders.
    Nalmefene Sulfate-d<sub>3</sub>
  • HY-144497
    HE-S2
    		Activator
    HE-S2 is an antibody-drug conjugate triggering a potent antitumor immune response. HE-S2 acts by blocking the PD-1/PD-L1 interaction and activating the Toll-like receptor 7/8 (TLR7/8) signaling pathway. HE-S2 has remarkable antitumor activity.
    HE-S2
  • HY-159743
    M101
    M101 is a vaccine adjuvant and a key component in vaccines. Adjuvants can be divided into immunostimulants and delivery systems. Adjuvants can not only enhance the intensity and durability of immune responses, but also affect the type of immune responses. On the one hand, immunostimulants promote the production of antigen signals and co-stimulatory signals by targeting Toll-like receptors (TLRs) and other pattern recognition receptors (PRRs), leading to the maturation and activation of antigen presenting cells (APCs), thereby enhancing adaptive immune responses; on the other hand, delivery systems are carrier materials that promote antigen delivery by prolonging the bioavailability of loaded antigens and targeting antigens to lymph nodes or APCs. Several common adjuvants include: saponins, TLRs agonists, polysaccharides, nanoparticles, cytokines, and mucosal adjuvants.
    M101
  • HY-159100
    PVP-037
    		Agonist
    PVP-037 is a potent TLR7 and TLR8 agonist adjuvant. PVP-037 shows broad innate immune activation and enhances vaccine immune responses .
    PVP-037
  • HY-155801
    CRX 527
    		Ligand
    CRX 527 is a ligand of TLR4 and also serves as an adjuvant for peptide-based cancer vaccines, showing potential to enhance anti-tumor immune responses. CRX 527 can also induce HSC differentiation, increase the proportion and quantity of LSK cells, and promote their differentiation into macrophages, activating immune defense and protecting intestinal epithelium from radiation damage.
    CRX 527
  • HY-145885
    TLR7/8 agonist 6
    		Agonist
    TLR7/8 agonist 6 (Compound 4) is the potent agonist of TLR7/8 with IC50s of 0.18 and 5.34 μM, respectively. TLR7/8 agonist 6 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for researching infectious disease, cancer, and autoimmune disorders.
    TLR7/8 agonist 6
  • HY-107352S
    Fosfenopril-d7
    Fosfenopril-d7 is deuterium labeled Fosfenopril.
    Fosfenopril-d<sub>7</sub>
  • HY-150212A
    Tilsotolimod sodium
    		Inhibitor
    Tilsotolimod (sodium) is a synthetic Toll-like receptor 9 (TLR9) agonist that has demonstrated antitumor activity in preclinical models.
    Tilsotolimod sodium
  • HY-P1405
    Pam3CSK4-Biotin
    		Agonist
    Pam3CSK4-Biotin is biotinylated Pam3CSK4. Pam3CSK4-Biotin is a Toll-like receptor 1/2 (TLR1/2) agonist.
    Pam3CSK4-Biotin
  • HY-172967
    SARM1-IN-5
    		Inhibitor
    SARM1-IN-5 (compound 1-23-a) is a SARM1 inhibitor. SARM1-IN-5 can be used in the study of axonal degeneration related diseases such as Alzheimer’s disease, Parkinson’s disease, amyotrophic lateral sclerosis (ALS), and multiple sclerosis (MS).
    SARM1-IN-5
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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