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-RS14584
    Tlr3 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Tlr3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Tlr3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Tlr3 Mouse Pre-designed siRNA Set A
    Tlr3 Mouse Pre-designed siRNA Set A
  • HY-159753
    HS105
    		Activator
    HS105 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.
    HS105
  • HY-173276
    SARM1-IN-4
    		Inhibitor
    SARM1-IN-4 (Compound 7) is an orally active SARM1 inhibitor. After being orally administered at a dose of 50 mg/kg in a mouse model, it can reduce the level of plasma neurofilament light chain (NfL). SARM1-IN-4 prevents programmed axonal degeneration by inhibiting the NAD+ hydrolase activity of SARM1, and it can be used in research related to neurodegenerative diseases and neurological disorders (such as multiple sclerosis, amyotrophic lateral sclerosis, Parkinson's disease, and peripheral neuropathies, etc.).
    SARM1-IN-4
  • HY-158694
    TLR7 agonist 20
    		Agonist
    TLR7 agonist 20 (compound 23) is an imidazoquinoline analogue. TLR7 agonist 20 is a potent TLR7 specific agonist, with an EC50 value of 0.23 μM for hTLR7. TLR7 agonist 20 shows strong adjuvant activity on spike antibody levels which induces a strong T helper 1 (Th1) response with increase in IgG2b and IgG2c, in addition to IgG1.
    TLR7 agonist 20
  • HY-163398
    TLR7-IN-1
    		Inhibitor
    TLR7-IN-1 (compound 16-A) is a TLR7 inhibitor with an EC50 value of 0.001 µM.
    TLR7-IN-1
  • HY-170899
    TLR7 agonist 28
    		Agonist
    TLR7 agonist 28 (compound 3) is a potent TLR7 agonist. TLR7 agonist 28 can conjugat to antitumor monoclonal antibodies (mAbs) for cancer immunotherapy.
    TLR7 agonist 28
  • HY-150740A
    ODN 21595 sodium
    		Inhibitor
    ODN 21595 sodium is a Guanine-Modified TLR7 and TLR9 inhibitor. ODN 21595 sodium inhibits the release of IFN-α and IL-6 with no cytotoxic. ODN 21595 sodium reduces the expression of CD86 and HLA-DR. ODN 21595 sodium has the potential for the research of systemic lupus erythematosus (SLE).
    ODN 21595 sodium
  • HY-159670B
    Monophosphoryl Lipid A-12 triethylamine
    		Agonist
    Monophosphoryl Lipid A-12 (triethylamine) is a toll-like receptor 4 agonist. Monophosphoryl Lipid A-12 (triethylamine) can be used for the research of immunization and vaccine.
    Monophosphoryl Lipid A-12 triethylamine
  • HY-B1370S
    Hydroxychloroquine-d4 sulfate
    		Inhibitor
    Hydroxychloroquine-d4 (sulfate) is the deuterium labeled Hydroxychloroquine sulfate. 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-d<sub>4</sub> sulfate
  • HY-147310
    CU-CPD107
    		Agonist 98.07%
    CU-CPD107 is a potent, selective toll-like receptor 8 (TLR 8) agonist. CU-CPD107 inhibits TLR8 signaling. CU-CPD107 converts to synergistic agonist activities in the presence of ssRNA and induces TLR8 signaling. CU-CPD107 inhibits proinflammatory factor expression and avoids immune responses in the presence of ssRNA.
    CU-CPD107
  • HY-170489
    Antifungal agent 123
    		Inhibitor
    Antifungal agent 123 (Compound 4b) exhibits good affinity to the oxidoreductase of Staphylococcus aureus or the membrane protein of Candida albicans, exhibits antibacterial and antifungal activities. Antifungal agent 123 scavenges free radical, exhibits antioxidant efficacy. Antifungal agent 123 inhibits the TLR signaling pathway, and exhibits anti-inflammatory efficacy.
    Antifungal agent 123
  • HY-145255
    Tri(TLR4-IN-C34-C2-amide-C3-amide-PEG1)-amide-C3-COOH
    		Inhibitor
    Tri(TLR4-IN-C34-C2-amide-C3-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-C3-amide-PEG1)-amide-C3-COOH
  • HY-P1181
    Pam2CSK4
    		Agonist
    Pam2CSK4, a lipopeptide, is a TLR6-independent TLR2 ligand and agonist. Pam2CSK4 promotes platelet aggregation, and increases platelet adhesion to collagen-coated surfaces in a TLR2/NF-κB/BTK-dependent manner. Pam2CSK4 also activates iNOS expression and NO production in mouse macrophages.
    Pam2CSK4
  • HY-D1056B1
    Lipopolysaccharides, from Proteus vulgaris
    Lipopolysaccharides, from Proteus vulgaris are lipopolysaccharide endotoxins and TLR-4 activators derived from Proteus vulgaris, 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 vulgaris exhibit a typical three-part structure: O-antigen, core oligosaccharide, and lipid A. Lipopolysaccharides, from Proteus vulgaris possess a unique molecular structure and chitosan affinity (Kb=2.72 μM), surpassing that of Yersinia pseudotuberculosis (Kb=6.06 μM) and Escherichia coli (Kb=79.50 μM).
    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 vulgaris
  • HY-103639
    M62812 free base
    		Inhibitor
    M62812 (free base) is a toll-like receptor 4 (TLR4) signal transduction inhibitor. M62812 can suppress endothelial cell and leukocyte activation and prevents lethal septic shock in mice. M62812 can be used for the research of sepsis.
    M62812 free base
  • HY-159672A
    3D-Monophosphoryl Lipid (12,16) free acid
    		Agonist
    3D-Monophosphoryl Lipid (12,16) (3D-MPL (12,16)) free acid is a TLR agonist that can be used as a vaccine adjuvant to enhance the immunogenicity of vaccines.
    3D-Monophosphoryl Lipid (12,16) free acid
  • HY-168207
    TH023
    		Inhibitor
    TH023 is an inhibitor for the TLR4 signaling pathway, that targets especially the formation of TLR4 homodimer. TH023 inhibits secreted embryonic alkaline phosphatase in cell HEK-Blue hTLR4 with an IC50 of 0.354 μM, and inhibits the NO expression in RAW264.7 with an IC50 of 1.61μM. TH023 also inhibits the activation of NF-κB, reduces the nuclear translocation of NF-κB p65. TH023 exhibits anti-inflammatory efficacy in LPS (HY-D1056)-induced mouse acute sepsis model, and ameliorates the mouse lung injury.
    TH023
  • HY-146244B
    FITC-labeled Agatolimod sodium
    		Agonist
    FITC-labeled Agatolimod (sodium), a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. FITC-labeled Agatolimod (sodium) can be used to evaluate CpG ODN cellular uptake and localization by confocal laser-scanning microscopy (excitation 495 nm, emission 520 nm) or flow cytometry.
    FITC-labeled Agatolimod sodium
  • HY-173070
    TLR7 agonist 29
    		Agonist
    TLR7 agonist 29 (Compound 1) is the agonist for TLR7 with an EC50 of 5.2 nM for human TLR7 (EC50 for mouse TLR7 is 48.2 nM). TLR7 agonist 29 activates bone marrow-derived macrophages (BMDMs), stimulates myeloid cells in the tumor microenvironment, promotes the expression of PD-L1, CD86 and IFN-α. TLR7 agonist 29 can be used as payload for synthesis of ADC.
    TLR7 agonist 29
  • HY-B1370E
    (R)-Hydroxychloroquine phosphate
    		Control
    (R)-Hydroxychloroquine ((R)-HCQ) phosphate is a (R)-isomer of Hydroxychloroquine (HY-W031727). (R)-Hydroxychloroquine inhibits the insulin metabolizing enzyme of cytosolic fraction of liver homogenates in healthy and diabetic rats.
    (R)-Hydroxychloroquine phosphate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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