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-Y0278
    Chloranil
    		Inducer 98%
    Chloranil (Tetrachloro-p-benzoquinone), an orally active metabolite of pentachlorophenol and hexachlorobenzene, is a widely used fungicide. Chloranil can induce ROS production. Chloranil induces neutrophil extracellular traps through the ROS-JNK-NOX2 pathway. Chloranil induces ferroptosis and neuroinflammation. Chloranil induces apoptosis of mouse embryonic stem cells .
    Chloranil
  • HY-126154
    L48H37
    		Inhibitor
    L48H37 is an analog of Curcumin (HY-N0005) with improved chemical stability. L48H37 is a potent and specific myeloid differentiation protein 2 (MD2) inhibitor and inhibits the interaction and signaling transduction of LPS-TLR4/MD2. L48H37 is used for the research of sepsis or lung injury treatment.
    L48H37
  • HY-150217A
    CpG ODN 10101 sodium
    		98.84%
    CpG ODN 10101 sodium, a synthetic oligodeoxynucleotide (ODN), is a toll-like receptor 9 (TLR9) agonist. CpG ODN 10101 sodium is a potent inducer of cytokine/chemokine expression ex vivo when used in combination with HH2(VQLRIRVAVIRA-NH2). CpG ODN 10101 sodium induces IFN- secretion from dendritic cells (DCs) and stimulates B-cells.CpG ODN 10101 sodium has antiviral and immunomodulatory properties that can influence chronic infection with HCV.
    CpG ODN 10101 sodium
  • 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-D1056A2
    Lipopolysaccharides, from E. coli O127:B8
    		Activator
    Lipopolysaccharides, from E. coli O127:B8 (LPS, from Escherichia coli (O127:B8)) are endotoxins and TLR4 activators extracted from Escherichia coli (E. coli O127:B8) and are classified as S (smooth) type LPS. Lipopolysaccharides, from E. coli O127:B8 possess the typical three-part structure: O-antigen, R3-type core oligosaccharide, and lipid A. Lipopolysaccharides, from E. coli O127:B8 activate TLR-4 in immune cells, can induce inflammatory responses and ileal contractility, and can be used to construct intestinal inflammation models.
    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 O127:B8
  • HY-153879
    C12-TLRa
    		Ligand ≥99.0%
    C12-TLRa is an ionized adjuvant lipid. C12-TLRa targets TLR7/8 receptors in endosomes. C12-TLRa enhances mRNA delivery as a structural component of LNPs. C12-TLRa enhances innate immune responses. C12-TLRa can be used for the research of SARS-CoV-2 mRNA vaccine.
    C12-TLRa
  • HY-W105835
    Magnesium citrate
    		Modulator ≥98.0%
    Magnesium citrate (Trimagnesium dicitrate) is an orally active magnesium-containing compound that can cross the blood-brain barrier (BBB). Magnesium citrate can be used as an intestinal cleanser and is studied for its application in laxatives. Magnesium citrate can also increase the pain threshold and is studied for pain-relief purposes.
    Magnesium citrate
  • HY-109010
    Poseltinib
    		Inhibitor 98.08%
    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-128598
    MD2-TLR4-IN-1
    		Inhibitor 98.16%
    MD2-TLR4-IN-1 is a myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex antagonist. MD2-TLR4-IN-1 inhibits Lipopolysaccharides (HY-D1056) (LPS)-induced expression of TNF-α and IL-6 in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively. MD2-TLR4-IN-1 can be used for the study of acute lung injury (ALI).
    MD2-TLR4-IN-1
  • HY-P99555
    Tomaralimab
    		Inhibitor
    Tomaralimab (OPN-305) is a humanized anti-TLR2 IgG4 monoclonal antibody. Tomaralimab inhibits TLR2, MyD88, NLRP3, and reduces pro-inflammatory cytokine (IL-1β, IL-6, IL-8) production. Tomaralimab reduces tau pathology. Tomaralimab improves cognition, atopic dermatitis. Tomaralimab has anticancer effects on pancreatic ductal adenocarcinoma. Tomaralimab is being studied in myelodysplastic syndrome (MDS), atopic dermatitis, pancreatic ductal adenocarcinoma, Alzheimer's disease, and myocardial ischemia/reperfusion injury.
    Tomaralimab
  • HY-N2110
    Phellopterin
    		Inhibitor 99.94%
    Phellopterin, an orally active furocoumarin with multiple biological activities. Phellopterin is a partial agonist of the central benzodiazepine receptors. Phellopterin exerts anti-inflammatory effects by upregulating SIRT1, downregulating ICAM-1 (reducing chronic inflammation, aiding diabetic ulcer healing), inhibiting STAT3 phosphorylation (easing atopic dermatitis inflammation), regulating Akt/PKC pathways (lowering TNF-α-induced VCAM-1 to block monocyte adhesion), and inhibiting TLR4/NF-κB pathway and macrophage M2 polarization (alleviating colitis-related cancers). Phellopterin suppresses ovarian cancer progression via inhibiting the PU.1/CLEC5A/PI3K-AKT loop (inducing cell cycle arrest, apoptosis, DNA damage). Phellopterin alleviates murine diabetes by promoting adipocyte differentiation and increasing PPARγ. Phellopterin also has anti-HSV-1 activity. Phellopterin can be used for studying anti-inflammation, anti-cancer (e.g., ovarian cancer, colitis cancer), blood glucose lowering, anti-diabetes, and anti-virus.
    Phellopterin
  • HY-N1508
    Ecliptasaponin A
    		Inhibitor 99.50%
    Ecliptasaponin A is an orally active pentacyclic triterpenoid saponin. Ecliptasaponin A exerts anti-tumor activity by activating ASK1/JNK pathway, inducing apoptosis and autophagy in lung cancer cells. Ecliptasaponin A exerts anti-inflammatory/anti-fibrotic effects and protects the cardiovascular system by inhibiting the HMGB1/TLR4/NF-κB pathway, and the expression of COX-2 and MMP-9. Ecliptasaponin A can enhance SOD activity, reduce MDA levels, and alleviate oxidative stress damage. Ecliptasaponin A exerts chondroprotective effects by inhibiting the expression of MMP13 and regulating inflammatory factors. Ecliptasaponin A improves ovarian function and regulates sex hormones by upregulating the expression of ESR1 receptors.
    Ecliptasaponin A
  • 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-B0180B
    Imiquimod maleate
    		Agonist 99.25%
    Imiquimod maleate (R 837 maleate), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod maleate exhibits antiviral and antitumor effects in vivo. Imiquimod maleate can be used for the research of external genital, perianal warts, cancer and COVID-19.
    Imiquimod maleate
  • 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
  • HY-118250
    GSK2245035
    		Agonist 99.85%
    GSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 is used for asthma.
    GSK2245035
  • HY-135905
    CL264
    		Inhibitor 98.63%
    CL264 is a TLR7-specific agonist for innate immune signals research.
    CL264
  • 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-153840A
    ODN INH 18 sodium
    		Inhibitor 99.76%
    ODN INH-18 sodium is a linear 24-mer class B INH-ODN in which the 5' INH-ODN 4084-F sequence was followed by a random stretch of 12 nucleotides lacking the ability to form significant secondary structures. ODN INH-18 sodium showes inhibitory potency for TLR9 ligand-induced IFN-α production.
    ODN INH 18 sodium
  • HY-B0012A
    Pamidronate disodium
    		Inhibitor ≥98.0%
    Pamidronate disodium (CGP 23339A), the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronate disodium significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of osteoprotegerin in cartilage and subchondral bone, and inhibiting the expression of RANKL and MMP-9 in both tissues, as well as TLR-4 in cartilage, thereby alleviating cartilage degeneration. Additionally, Pamidronate disodium can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma.
    Pamidronate disodium
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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