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-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-B0380A
    Trimebutine maleate
    		Inhibitor 99.91%
    Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate 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 maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
    Trimebutine maleate
  • HY-138139B
    AXC-715 trihydrochloride
    		Agonist 99.76%
    AXC-715 (T785) trihydrochloride is a TLR7/TLR8 dual agonist. AXC-715 trihydrochloride can be used for synthesis of antibody-adjuvant immunoconjugates, comprising an antibody construct that binds programmed death-ligand 1 (PD-L1) linked to one or more adjuvants.
    AXC-715 trihydrochloride
  • HY-112051
    CU-CPT9b
    		Antagonist 99.03%
    CU-CPT9b is a specific TLR8 antagonist, with an IC50 of 0.7 nM. CU-CPT9b shows high binding affinity towards TLR8 with a Kd of 21 nM.
    CU-CPT9b
  • HY-144501
    D18
    		Agonist 98.79%
    D18 is an immune modulator. D18 acts as a TLR7/8 dual agonist (EC50=24 nM for hTLR7 and 10 nM for hTLR8, respectively). D18 increases PD-L1 expression through epigenetic regulation, thus sensitizing tumors to PD-1/PD-L1 blockade. D18 is a ADC cytotoxin uesd for the systhesis of ADC HE-S2.
    D18
  • HY-P10208A
    RKH acetate
    		Antagonist 99.45%
    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-131945
    CU-115
    		Antagonist 99.63%
    CU-115 is a potent TLR8 antagonist (IC50=1.04 µM), and shows selective for TLR8 over TLR7 (IC50=>50 µM). CU-115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells.
    CU-115
  • HY-D1056A3
    Lipopolysaccharides, from E. coli O26:B6
    		Activator
    Lipopolysaccharides, from E. coli (Escherichia coli) O26:B6 are lipopolysaccharide endotoxins and TLR-4 activators derived from E. coli, 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 E. coli O26:B6 exhibit a typical three-part structure: O-antigen (O-antigen), core oligosaccharide (core oligosaccharide), and lipid A (Lipid A), and can be recognized by the core-specific monoclonal antibody MAb J8-4C10. Lipopolysaccharides, from E. coli O26:B6 can promote an increase in pro-inflammatory cytokines in plasma, thereby triggering hypothalamic-pituitary-adrenal (HPA) activation and leading to adrenal oxidative damage. The pathogenic effects of Lipopolysaccharides, from E. coli O26:B6 can be blocked by PD149163 (HY-123434).
    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 E. coli O26:B6
  • 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 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 P. aeruginosa 10
  • HY-13740G
    Resiquimod (GMP)
    		Agonist
    Resiquimod (R848) (GMP) is Resiquimod (HY-13740) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist. Resiquimod (GMP) can induce human mMDSC to mature into inflammatory macrophages.
    Resiquimod (GMP)
  • HY-128799A
    CL097 hydrochloride
    		Agonist 99.96%
    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-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-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 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 S. marcescens
  • HY-117602
    TLR7 agonist 3
    		Agonist 99.90%
    TLR7 agonist 3 (compound 2) is a TLR7 agonist. TLR7 agonist 3 (compound 5) can be coupled to folate receptor binding ligands to target myeloid-derived suppressor cells and exert anticancer activity.
    TLR7 agonist 3
  • HY-153254
    BMS905
    		Inhibitor 99.59%
    BMS905 is an orally active TLR7 and TLR8 dual inhibitor (IC50s: 0.7 and 3.2 nM respectively). BMS905 inhibits TLR7 or TLR8 induced IL-6 production in human/mouse whole blood. BMS905 can be used for research of lupus.
    BMS905
  • 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-125390
    SM-360320
    		Agonist 99.41%
    SM-360320 (CL-087) is a potent, orally active TLR7 agonist. SM-360320 is a immuno-modulator and exerts an antitumor effect. SM-360320 can act in synergy with DNA vaccines leading to an enhanced Th1 antibody response. SM-360320 can inhibit HCV replication in hepatocytes via a type I IFN-independent mechanism in addition to its IFN-mediated activity.
    SM-360320
  • HY-146244A
    Biotin-labeled Agatolimod sodium
    Biotin-labeled Agatolimod (sodium), a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. Biotin-labeled Agatolimod (sodium) can be used to evaluate CpG ODN cellular uptake and localization using a biotin detection system and light microscopy.
    Biotin-labeled Agatolimod sodium
  • HY-N0392
    Polygalasaponin F
    		Inhibitor 99.85%
    Polygalasaponin F, an oleanane-type triterpenoid saponin extracted from Polygala japonica, decreases the release of the inflammatory cytokine tumor necrosis factor a (TNFa). Polygalasaponin F reduces neuroinflammatory cytokine secretion through the regulation of the TLR4-PI3K/AKT-NF-kB signaling pathway .
    Polygalasaponin F
  • HY-N4093
    Astringin
    		Inhibitor 99.54%
    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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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