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-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-107352
    Fosfenopril
    		Inhibitor 99.85%
    Fosfenopril (Fosinoprilat) is a potent angiotensin converting enzyme (ACE) inhibitor. Fosfenopril alleviates lipopolysaccharide (LPS)-induced inflammation by inhibiting TLR4/NF-κB signaling in monocytes.
    Fosfenopril
  • HY-156174
    E104
    		Inhibitor 98.02%
    E104 (compound 1) is a potent and selective TLR7 agonist. E104 can be delivered by antibody-drug conjugate (ADC) technology to elicit potent anticancer activity. E104 induces the activation of mouse macrophages and hPBMCs.
    E104
  • HY-150746
    ODN 24991
    		Inhibitor
    ODN 24991, a guanine-modified inhibitory oligonucleotide (INH-ODN), is a TLR3, TLR7 and TLR9 (Toll-like receptor) inhibitor, and its parent is INH-ODN 2088. ODN 24991 disrupts TLR3-, TLR7- and TLR9-mediated immune cell immune responses. ODN 24991 sequence: 5'-C-C-T-G-G-C-c7rGm-G-G-G-3'.
    ODN 24991
  • HY-P10586A
    Macrophage-activating lipopeptide 2 TFA
    		Activator 98.60%
    Macrophage-activating lipopeptide 2 TFA is an agonist of Toll like receptors TLR-2/TLR-6. Macrophage-activating lipopeptide-2 enhances endothelial nitric oxide synthase (eNOS) phosphorylation and endothelial cell release of NO, thereby improving vasodilation. Macrophage-activating lipopeptide-2 enhances endothelial adhesion of white blood cells and improve perfusion recovery and collateral growth in the hind limbs of hypercholesterolemic Apoe deficient mice undergoing experimental femoral artery ligation (FAL).
    Macrophage-activating lipopeptide 2 TFA
  • HY-137345
    DB-3-291
    		Inhibitor 98.56%
    DB-3-291 is potent and selective PROTAC CSK degrader, with a Kd of 1 nM (Pink: CSK ligand (HY-131669); Blue: E3 ligase ligand (HY-103597); Black: linker (HY-N2407)).
    DB-3-291
  • HY-160227A
    ORN 06 sodium
    		Activator
    ORN 06 (sodium) s a synthetic single-stranded U-rich RNA and contains 6 repeats of the UUGU sequence motif. The GU-rich oligoribonucleotides (ORNs) are able to stimulate TLR7.
    ORN 06 sodium
  • 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-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-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-B0380
    Trimebutine
    		Inhibitor 99.42%
    Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine 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 also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
    Trimebutine
  • HY-111786
    LHC-165
    		Agonist ≥98.0%
    LHC-165 is a TLR7 agonist. LHC-165 has potential to used in study of solid tumors.
    LHC-165
  • HY-107744
    Nalmefene
    		Inhibitor 99.70%
    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-N6928
    Mogroside III-E
    		99.32%
    Mogroside III-E is a cucurbitane-type compound isolated from Siraitia grosvenorii, inhibits NO release, with anti-fibrotic activity.
    Mogroside III-E
  • 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-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-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-145645
    Paridiprubart
    		Inhibitor
    Paridiprubart (NI-0101) is a humanised anti-TLR4 monoclonal antibody. Paridiprubart has the potential for the research of rheumatoid arthritis.
    Paridiprubart
  • HY-150743A
    Biotin-labeled ODN 2395 sodium
    Biotin-labeled ODN 2395 (sodium), a C class oligodeoxynucleotide, is a TLR9 agonist. Biotin-labeled ODN 2395 (sodium) can be used to evaluate CpG ODN cellular uptake and localization using a biotin detection system and light microscopy.
    Biotin-labeled ODN 2395 sodium
  • HY-150746A
    ODN 24991 sodium
    		99.64%
    ODN 24991 sodium, a guanine-modified inhibitory oligonucleotide (INH-ODN), is a TLR3, TLR7 and TLR9 (Toll-like receptor) inhibitor, and its parent is INH-ODN 2088. ODN 24991 sodium disrupts TLR3-, TLR7- and TLR9-mediated immune cell immune responses. ODN 24991 sequence: 5'-C-C-T-G-G-C-c7rGm-G-G-G-3'.
    ODN 24991 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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