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-124750
    NecroX-7
    		Inhibitor 99.69%
    NecroX-7 is a potent free radical scavenger and a HMGB1 (high-mobility group box 1) inhibitor. NecroX-7 can be used as an antidote to acetaminophen toxicity. NecroX-7 exerts a protective effect by preventing the release of HMGB1 in ischemia/reperfusion injury. NecroX-7 inhibits the HMGB1-induced release of TNF and IL-6, as well as the expression of TLR-4 and receptor for advanced glycation end products. NecroX-7 can be used graft-versus-host disease (GVHD) research.
    NecroX-7
  • HY-D1056C3
    Lipopolysaccharides, from S. enterica serotype typhimurium
    		Activator
    Lipopolysaccharides, from S. enterica (Salmonella enterica) serotype typhimurium are lipopolysaccharide endotoxins and TLR4 activators derived from serotype typhimurium of Salmonella enterica, and are classified as S-type LPS. Lipopolysaccharides, from S. enterica exhibit a typical three-part structure: O-antigen, core oligosaccharide, and lipid A. Lipopolysaccharides, from S. enterica serotype typhimurium can modulate the fate of bacteria in dendritic cells (DC), determining the uptake, degradation, and activation of immune functions by DC cells against the bacteria.
    It is recommended to prepare a solution with concentration ≥2 mg/mL. Vortex thoroughly for more than 10 minutes. Due to the adsorption characteristics of LPS, silanized container or low adsorption centrifuge tubes should be used for aliquoting and storage, and mix thoroughly before use.
    Lipopolysaccharides, from S. enterica serotype typhimurium
  • HY-P10208A
    RKH acetate
    		Antagonist 99.79%
    RKH acetate exerts protective effects against sepsis-induced death and organ damage. RKH acetate can directly bind to Toll-like receptor 4 (TLR4) and block TLR4 signal transduction in immune cells.
    RKH acetate
  • HY-D1056E
    Lipopolysaccharides, from P. aeruginosa 10
    		Activator
    Lipopolysaccharides from P. aeruginosa (Pseudomonas aeruginosa) 10 are lipopolysaccharide endotoxins and TLR4 activators derived from Pseudomonas aeruginosa 10, and are classified as S-type LPS. Lipopolysaccharides from P. aeruginosa 10 exhibit a typical three-part structure: O-antigen, core oligosaccharide, and lipid A. The lipopolysaccharides of P. aeruginosa 10 have a fatty acid composition distinct from common enterobacteria, an exceptionally high degree of phosphorylation (triphosphate residues have been detected), and a unique outer region of the core oligosaccharide. Additionally, their O-specific side chains are typically rich in novel aminosugars. Lipopolysaccharides from P. aeruginosa 10 demonstrate susceptibility to viruses, with the level of susceptibility determined by the content of high molecular weight polysaccharides in their composition. The absence of high molecular weight polysaccharides increases their sensitivity to bacteriophages.
    It is recommended to prepare a solution with concentration ≥2 mg/mL. Vortex thoroughly for more than 10 minutes. Due to the adsorption characteristics of LPS, silanized container or low adsorption centrifuge tubes should be used for aliquoting and storage, and mix thoroughly before use.
    Lipopolysaccharides, from P. aeruginosa 10
  • HY-120538
    CPG-52364
    		Antagonist 99.20%
    CPG-52364 (compound 2) is a TLR9 antagonist. CPG-52364 inhibits the HEK293-hTLR9 cell with an IC50 value of 4.6 nM.
    CPG-52364
  • HY-107744
    Nalmefene
    		Inhibitor 99.94%
    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
  • HY-N6612R
    D-Glucuronic acid (Standard)
    		Agonist
    D-Glucuronic acid (Standard) is the analytical standard of D-Glucuronic acid. This product is intended for research and analytical applications. D-Glucuronic acid is a major component of many anti-inflammatory proteoglycans, which can promote embryonic development and inhibit cell aggregation. After being metabolized into ethyl glucuronide (HY-113093), D-Glucuronic acid activates Toll-like receptor 4 (TLR4), causing pain. D-Glucuronic acid and its derivative glucurono-lactone can serve as liver detoxifiers for human health prevention, and its derivatives also possess anti-tumor activity.
    D-Glucuronic acid (Standard)
  • HY-D1056H
    Lipopolysaccharides, from S. marcescens
    		Activator
    Lipopolysaccharides, from S. marcescens (Serratia marcescens) are lipopolysaccharide endotoxins and TLR-4 activators derived from Serratia marcescens, 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 S. marcescens exhibit a typical three-part structure: O-antigen (O-antigen), core oligosaccharide (core oligosaccharide), and lipid A (Lipid A). Lipopolysaccharides, from S. marcescens induce NF-κB activation in mouse cells via Toll-like receptor (TLR4)/MD-2. The lipopolysaccharides of S. marcescens can induce apoptosis in host immune cells, thereby suppressing the host's innate immunity.
    It is recommended to prepare a solution with concentration ≥2 mg/mL. Vortex thoroughly for more than 10 minutes. Due to the adsorption characteristics of LPS, silanized container or low adsorption centrifuge tubes should be used for aliquoting and storage, and mix thoroughly before use.
    Lipopolysaccharides, from S. marcescens
  • HY-108910A
    Chymotrypsin (MS grade)
    		Inhibitor
    Chymotrypsin (EC 3.4.21.1; Chymotrypsin A) (MS grade) is an orally effective inhibitor targeting molecules such as TLR4, NF-κB, MMP-1, TNF-α, IL-1β, and IL-6. Chymotrypsin (MS grade) downregulates the TLR4/NF-κB signaling pathway, inhibits the release of inflammatory factors, reduces cell infiltration and tissue damage, and also reduces the expression of tumor cell adhesion molecules (such as CD44 and CD54). It can also be specifically detected by fluorescent probes (such as NBD-3). Chymotrypsin (MS grade) has anti-inflammatory, hepatoprotective, joint damage-reducing, liver protection against lipotoxicity, and anti-tumor metastasis functions, and can be used in the research of diseases such as rheumatoid arthritis, non-alcoholic fatty liver disease, and melanoma metastasis. Chymotrypsin (MS grade) can be used in studies of inflammation, edema, and expectoration.
    Chymotrypsin (MS grade)
  • HY-111582
    BBIQ
    		Agonist 99.81%
    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-145645
    Paridiprubart
    		Inhibitor
    Paridiprubart (NI-0101) is a humanised anti-TLR4 monoclonal antibody. Paridiprubar inhibits the production of pro-inflammatory cytokines by monocytes from rheumatoid arthritis specimen induced by rheumatoid arthritis synovial fluid (RASF). Paridiprubart can be used for the study of rheumatoid arthritis.
    Paridiprubart
  • HY-B1370R
    Hydroxychloroquine sulfate (Standard)
    		Inhibitor
    Hydroxychloroquine (sulfate) (Standard) is the analytical standard of Hydroxychloroquine (sulfate). This product is intended for research and analytical applications. Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro.
    Hydroxychloroquine sulfate (Standard)
  • HY-150217
    CpG ODN 10101
    		Agonist 99.44%
    CpG ODN 10101 (ODN 10101; CPG 10101) is a selective agonist targeting TLR9, a synthetic oligodeoxynucleotide modified with phosphate thioester. CpG ODN 10101 activates B cells and plasmacytoid dendritic cells (pDCs), inducing the production of cytokines and chemokines such as interferon-IFN-α, interferon-inducible protein IP-10, and 2'5'-oligoadenylate synthase (2'5'-OAS), regulating innate immunity and promoting Th1 adaptive immune responses. CpG ODN 10101 also possesses antiviral properties and enhances vaccine immunogenicity, making it suitable as an immunomodulator and vaccine adjuvant for vaccine development in chronic hepatitis C and infectious diseases such as melioidosis, pertussis, and respiratory syncytial virus (RSV).
    CpG ODN 10101
  • HY-109010
    Poseltinib
    		Inhibitor 98.11%
    Poseltinib (HM71224) is an orally active, selective, irreversible small molecule Bruton tyrosine kinase (BTK) inhibitor. With an IC50 of 1.95 nM. Poseltinib effectively inhibits the signaling mediated by B cell receptors (BCR), Fc receptors (FcR), and Toll-like receptors (TLR). Poseltinib has anti-inflammatory activity and can be used in the research of rheumatoid arthritis.
    Poseltinib
  • HY-101929
    CU-CPT17e
    		Agonist 98.67%
    CU-CPT17e is a potent multi-Toll-like receptor (TLR) agonist that activates TLR3, TLR8, and TLR9.
    CU-CPT17e
  • HY-130797
    TLR7/8 agonist 3
    		Agonist 99.96%
    TLR7/8 agonist 3 (Compound II) is a potent TLR7 and TLR8 agonist, extracted from patent WO2016057618 (compound of formula (II)).
    TLR7/8 agonist 3
  • HY-101318
    β-Funaltrexamine hydrochloride
    		Inhibitor 99.07%
    β-Funaltrexamine (β-FNA) hydrochloride is a blood-brain barrier-permeable, selective and irreversible μ-opioid receptor antagonist with immunomodulatory, anti-inflammatory and neuroprotective activities. β-Funaltrexamine hydrochloride inhibits p38 MAPK and TLR4 signaling by blocking μ-opioid receptors, and reduces the transcriptional activities of NF-κB, AP-1, CREB and Stat. Furthermore, β-Funaltrexamine hydrochloride inhibits iNOS activation and pro-inflammatory microglial polarization, converting microglia to an anti-inflammatory phenotype, thereby downregulating neuroinflammation and ameliorating neuronal degeneration. β-Funaltrexamine hydrochloride is widely applicable to research related to stroke, cerebral ischemia/reperfusion injury and neurodegenerative diseases.
    β-Funaltrexamine hydrochloride
  • HY-N0726
    Dracorhodin perchlorate
    		Modulator 99.02%
    Dracorhodin perchlorate (Dracohodin perochlorate) is a natural product that can be obtained from the natural active molecule Dragon's blood. Dracorhodin perchlorate inhibits PI3K/Akt and NF-κB activation, upregulates p53 expression, activates caspase, produces ROS, and promotes Apoptosis. Dracorhodin perchlorate regulates the TLR4. Dracorhodin perchlorate promotes wound healing, improves diabetes. Dracorhodin perchlorate has anti-tumor activity against prostate cancer, breast cancer, cervical cancer and other cancers.
    Dracorhodin perchlorate
  • HY-B1900
    Methylprednisolone succinate
    		Inhibitor 99.67%
    Methylprednisolone succinate (Methylprednisolone hydrogen succinate) is a prodrug of Methylprednisolone (HY-B0260) and glucocorticoid with immunosuppressant and anti-inflammatory activity. Methylprednisolone succinate binds cytosolic glucocorticoid receptors, translocates to nuclei, and modulates target gene transcription. Methylprednisolone succinate alters Bax, Bcl-2, occludin, and ZO-1 expression; attenuates TLR4/NF-κB signaling; suppresses proinflammatory cytokine production and immune cell activation. Methylprednisolone succinate can be used for the research of intracranial haemorrhage, rheumatoid arthritis, multiple sclerosis, preterminal cancer, inflammatory conditions, shock, immediate-type hypersensitivity, acute myocardial ischemia, hypoxic heart muscle damage, and traumatic spinal cord injury.
    Methylprednisolone succinate
  • HY-148511A
    Vidutolimod sodium
    		Inhibitor
    Vidutolimod sodium is a CpG-A oligodeoxynucleotide. Vidutolimod sodium is a Toll-like receptor 9 (TLR9) agonist, which activates plasmacytoid dendritic cells (pDCs) and triggers interferon alpha (IFNα) release, leading to a cascade of anti-tumor immune effects.
    Vidutolimod sodium
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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