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-17007R
    Saquinavir (Standard)
    		Inhibitor
    Saquinavir (Standard) (Ro 31-8959 (Standard)) is the analytical standard of Saquinavir (HY-17007). This product is intended for research and analytical applications. Saquinavir (Ro 31-8959) is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir also has anti-inflammatory activity and can induce apoptosis of human red blood cells.
    Saquinavir (Standard)
  • HY-173388
    TLR4-IN-2
    		Inhibitor
    TLR4-IN-2 (Compound Racemic-11k) is inhibitors of TLR4, JNK, and NF-κB. TLR4-IN-2 inhibits NO production in LPS-stimulated RAW264.7 cells with an IC50 value of 23.2 µM. TLR4-IN-2 exerts anti-inflammatory activity by inhibiting TLR4 expression, reducing JNK phosphorylation, thereby suppressing the activation of NF-κB, blocking the transcription of inflammation-related genes, reducing the expression of iNOS and COX-2, and decreasing the production of inflammatory mediators such as NO, PGE 2, and TNF-α. TLR4-IN-2 is promising for research of inflammatory diseases, such as rheumatoid arthritis and various inflammatory disorders.
    TLR4-IN-2
  • HY-N0022R
    Isoacteoside (Standard)
    		Inhibitor
    Isoacteoside (Standard) is the analytical standard of Isoacteoside. This product is intended for research and analytical applications. Isoacteoside is a natural product that can significantly inhibit the formation of glycation end products. Isoacteoside Standard regulates the AKT/PI3K/m-TOR/NF-κB signaling pathway, induces apoptosis in OVCAR-3 cell. Isoacteoside Standard exhibits antitumor, anti-inflammatory, anti-obesity and neuroprotective activities.
    Isoacteoside (Standard)
  • HY-W014223R
    2,4′-Dihydroxybenzophenone (Standard)
    2,4′-Dihydroxybenzophenone (Standard) is the analytical standard of 2,4′-Dihydroxybenzophenone. This product is intended for research and analytical applications. 2,4′-Dihydroxybenzophenone (Ultraviolet absorber UV-0) occupies the hydrophobic pocket of MD2 and blocks the dimerization of TLR4. 2,4′-Dihydroxybenzophenone inhibits the LPS induced mtROS production, and LPS induced inflammatory response by downregulating pro-inflammatory mediators and decreasing the expression of MyD88, p-IRAK4, and NF-κB. 2,4′-Dihydroxybenzophenone is also a UV absorber.
    2,4′-Dihydroxybenzophenone (Standard)
  • HY-N0795R
    Procyanidin B1 (Standard)
    		Antagonist
    Procyanidin B1 (Standard) is the analytical standard of Procyanidin B1. This product is intended for research and analytical applications. Procyanidin B1 is a polyphenolic flavonoid isolated from commonly eaten fruits, binds to TLR4/MD-2 complex, and has anti-inflammatory activity.
    Procyanidin B1 (Standard)
  • HY-13655A
    Isatoribine
    		Agonist
    Isatoribine is a TLR7 agonist. Isatoribine is used in the study of chronic hepatitis C virus (HCV) infection.
    Isatoribine
  • HY-103697AR
    Gardiquimod diTFA (Standard)
    Gardiquimod (diTFA) (Standard) is the analytical standard of Gardiquimod (diTFA). This product is intended for research and analytical applications. Gardiquimod diTFA is an imidazoline TLR7/8 agonist. Gardiquimod diTFA inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 at concentrations below 10 μM.
    Gardiquimod diTFA (Standard)
  • HY-159914
    AYK004-B1
    		Agonist
    AYK004-B1 is a TLR7 agonist (EC50=0.2265 nM). AYK004-B1 can be used to prepare immune adjuvants.
    AYK004-B1
  • HY-103697R
    Gardiquimod (Standard)
    Gardiquimod (Standard) is the analytical standard of Gardiquimod. This product is intended for research and analytical applications. Gardiquimod is an imidazoline TLR7/8 agonist. Gardiquimod inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 at concentrations below 10 μM.
    Gardiquimod (Standard)
  • HY-W130878
    4-Octylphenol
    4-Octylphenol is a hormone disruptor that has gender-specific effects on male reproductive cells, significantly reducing the mitotic index and the number of spermatogonia. 4-Octylphenol can cause inflammatory damage to fish gills by activating the complement system through the C3a/C3aR axis and the C5a/C5aR1 axis, this leads to complement activation and causes immune suppression due to the imbalance between Th1/Th2 cells and regulatory T cells (Treg)/Th17 cells, as well as inflammatory damage via the Toll-like receptor 7 (Toll-like Receptor (TLR))/IκBα/NF-κB pathway.
    4-Octylphenol
  • HY-B0180R
    Imiquimod (Standard)
    		Agonist
    Imiquimod (Standard) is the analytical standard of Imiquimod. This product is intended for research and analytical applications. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19.
    Imiquimod (Standard)
  • HY-N1346R
    Robinin (Standard)
    		Inhibitor
    Robinin (Standard) is the analytical standard of Robinin. This product is intended for research and analytical applications. Robinin is a flavonoid that can be extracted from the leaves of purple cowpea, inhibiting TGF-β, TLR4/NF-κB and TLR2-PI3k-AKT signaling pathways. Robinin exerts anti-inflammatory and anti-tumor effects. The combination of Robinin and Methotrexate (HY-14519) reduces inflammation in experimental arthritis, Robinin can decrease the Doxorubicin (HY-15142A) induced cardiac toxicity effect.
    Robinin (Standard)
  • HY-B0180C
    Imiquimod dihydrochloride
    		Agonist
    Imiquimod (R 837) dihydrochloride, an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19.
    Imiquimod dihydrochloride
  • HY-D1056A4
    Lipopolysaccharides, from E. coli O128:B12
    		Activator
    Lipopolysaccharides, from E. coli O128:B12 (LPS, from Escherichia coli (O128:B12)) are endotoxins and TLR4 activators extracted from Escherichia coli (E. coli O128:B12) and are classified as S (smooth) type LPS. Lipopolysaccharides, from E. coli O128:B12 possess the typical three-part structure: O-antigen, R3-type core oligosaccharide, and lipid A. Lipopolysaccharides, from E. coli O128:B12 activate TLR-4 in immune cells, can be used to construct animal models of neonatal brain inflammation, and may influence preterm birth in neonates.
    Lipopolysaccharides, from E. coli O128:B12
  • HY-P10718
    IMG-2005
    		Inhibitor
    IMG-2005 is a TLR signaling pathway inhibitor. IMG-2005 mimics the Toll/interleukin-1 receptor (TIR) domain of MyD88, thereby preventing its homodimerization, which causes damage to tracheal epithelial cells and triggers pulmonary immune diseases.
    IMG-2005
  • HY-111582G
    BBIQ (GMP)
    		Agonist
    BBIQ (GMP) is BBIQ (HY-111582) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BBIQ is a potent and selectively toll-like receptor 7 (TLR7) agonist with an EC50 of  59.1 nM. BBIQ is a powerful vaccine adjuvant that enhances innate immune responses.
    BBIQ (GMP)
  • HY-159671A
    3D-Monophosphoryl Lipid (14) triethylamine
    		Agonist
    3D-Monophosphoryl Lipid (14) (3D-Monophosphoryl Lipid (14)) triethylamine is a TLR agonist that can be used as a vaccine adjuvant to enhance the immunogenicity of vaccines.
    3D-Monophosphoryl Lipid (14) triethylamine
  • HY-D1056D
    Lipopolysaccharides, from P. gingivalis
    Lipopolysaccharides, from P. gingivalis (LPS, from Porphyromonas gingivalis) are endotoxins and TLR4 activators extracted from Porphyromonas gingivalis (P. gingivalis) and are classified as S (smooth) type LPS. Lipopolysaccharides, from P. gingivalis possess the typical three-part structure: O-antigen, core oligosaccharide, and lipid A. Lipopolysaccharides, from P. gingivalis activate TLR-4 in immune cells and are important virulence factors in the mechanism of periodontal disease. Lipopolysaccharides, from P. gingivalis can be used in research related to periodontitis.
    Lipopolysaccharides, from P. gingivalis
  • HY-159672B
    3D-Monophosphoryl Lipid (12,16) triethylamine
    		Agonist
    3D-Monophosphoryl Lipid (12,16) (triethylamine) is a TLR agonist that can be used as a vaccine adjuvant to enhance the immunogenicity of vaccines.
    3D-Monophosphoryl Lipid (12,16) triethylamine
  • HY-162579
    TLR7 agonist 22
    		Agonist
    TLR7 agonist 22 (Compound 11a) emerges as a selective TLR7 agonist with an IC50 value of 25.86 μM. TLR7 agonist 22 inhibits the cellular HBsAg secretion and effectively activates TLR7, thereby inducing the secretion of TLR7-regulated cytokines IL-12, TNF-αand IFN-αin human PBMC cells. TLR7 agonist 22 is a promising for research in the field of developing novel immunomodulatory anti-HBV agents.
    TLR7 agonist 22
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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