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-116213
    Sparstolonin B
    		Antagonist 99.54%
    Sparstolonin B acts as a selective TLR2 and TLR4 antagonist and selectively blocks TLR2- and TLR4-mediated inflammatory signaling. Sparstolonin B has anti-HIV and anticancer activities.
    Sparstolonin B
  • HY-N6673
    Okanin
    		Inhibitor 99.98%
    Okanin, effective constituent of the flower tea Coreopsis tinctoria, attenuates LPS-induced microglial activation through inhibition of the TLR4/NF-κB signaling pathways.
    Okanin
  • HY-150726
    ODN 1668
    		Agonist
    ODN 1668, a class B CpG ODN (oligodeoxynucleotide), is a TLR-9 agonist. ODN 1668 has strong immune regulatory properties, can enhance the level of antibody IgG2 subtype, promote the immune response of T cells and B cells, and can be used in the study of vaccine adjuvants. In addition, CpG ODN 1668 induces an antimicrobial immune response via a CaTLR9 dependent pathway in groupers. Sequence: 5'-tccatgacgttcctgatgct-3’.
    ODN 1668
  • HY-N6612
    D-Glucuronic acid
    		Agonist
    D-Glucuronic acid is a major component of many anti-inflammatory proteoglycans, which can promote embryonic development and inhibit cell aggregation. After being metabolized into ethyl glucuronide (HY-113093), D-Glucuronic acid activates Toll-like receptor 4 (TLR4), causing pain. D-Glucuronic acid and its derivative glucurono-lactone can serve as liver detoxifiers for human health prevention, and its derivatives also possess anti-tumor activity.
    D-Glucuronic acid
  • HY-139413
    β-D-Glucan
    		≥98.0%
    β-D-glucan is a natural non-digestible polysaccharide and high biocompatibility that can be selectively recognized by recognition receptors such as Dectin-1 and Toll-like receptors as well as being easily internalized by murine or human macrophages, which is likely to attribute to a target delivery. β-d-glucan is an enteric delivery vehicle for probiotics.
    β-D-Glucan
  • HY-148045
    TLR9-IN-1
    		Inhibitor 99.80%
    TLR9-IN-1 is a potent and selective TLR9 inhibitor with an IC50 value of 7 nM for human TLR9. TLR9-IN-1 can be used for researching diseases associated with undesirable immune response.
    TLR9-IN-1
  • HY-150738
    ODN 2088
    		Antagonist
    ODN 2088 is a potent TLR3, TLR7 and TLR9 inhibitor. ODN 2088 shows no cytotoxic. ODN 2088 inhibits the release of IFN-α and IL-6.
    ODN 2088
  • HY-139323
    TLR7/8-IN-1
    		Inhibitor 99.92%
    TLR7/8-IN-1 is a crystalline from of a TLR7/TLR8 inhibitor extracted from patent WO2019220390, compound 2b. TLR7/8-IN-1 can be used for the research of autoimmune disease.
    TLR7/8-IN-1
  • HY-150726C
    ODN 1668 sodium
    		Agonist ≥99.0%
    ODN 1668 sodium, a class B CpG ODN (oligodeoxynucleotide), is a TLR-9 agonist. ODN 1668 sodium has strong immune regulatory properties, can enhance the level of antibody IgG2 subtype, promote the immune response of T cells and B cells, and can be used in the study of vaccine adjuvants. In addition, CpG ODN 1668 sodium induces an antimicrobial immune response via a CaTLR9 dependent pathway in groupers. Sequence: 5'-tccatgacgttcctgatgct-3’.
    ODN 1668 sodium
  • HY-103698A
    TLR7/8 agonist 1 dihydrochloride
    		Agonist 99.70%
    TLR7/8 agonist 1 dihydrochloride is a toll-like receptor TLR7/TLR8 dual-agonistic imidazoquinoline.
    TLR7/8 agonist 1 dihydrochloride
  • HY-N1346
    Robinin
    		Inhibitor 98.77%
    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
  • HY-N0625A
    Alpinetin
    		Inhibitor 99.51%
    Alpinetin is a flavonoid isolated from cardamom and possesses antitumor, antiinflammation, hepatoprotective, cardiovascular protective, lung protective, antibacterial, antiviral, neuroprotective properties. Alpinetin inhibits lipopolysaccharide (LPS)-induced inflammation, activates PPAR-γ, activates Nrf2, and inhibits TLR4 expression to protect LPS-induced renal injury.
    Alpinetin
  • HY-103697
    Gardiquimod
    		Agonist 99.91%
    Gardiquimod, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 when used at concentrations below 10?μM.
    Gardiquimod
  • HY-P1439A
    RS 09 TFA
    		Agonist 99.81%
    RS 09 TFA is a TLR4 agonist. RS 09 TFA promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. RS 09 TFA acts as an adjuvant in vivo; RS 09 TFA enhances X-15 specific antibody serum concentrations, when administered with X-15-KLH in mice.
    RS 09 TFA
  • HY-14806B
    Teneligliptin hydrobromide hydrate
    		Inhibitor 99.87%
    Teneligliptin (MP-513) hydrobromide hydrate is an orally active and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50s: 0.37 and 0.29 nM for the human and rat DPP-4, respectively). Teneligliptin hydrobromide hydrate improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus.
    Teneligliptin hydrobromide hydrate
  • HY-125171
    IAXO-102
    		Antagonist ≥98.0%
    IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. IAXO-102 inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein. IAXO-102 also prevents experimental abdominal aortic aneurysm development.
    IAXO-102
  • HY-145917
    SARM1-IN-2
    		Inhibitor 99.34%
    SARM1-IN-2 (Example 82) is a SARM1 inhibitor with an IC50 value of <1 μM. SARM1-IN-2 inhibits axonal regrowth, leading to only 6% regrowth after 72 h of exposure. SARM1-IN-2 can be used for the research of axonal degeneration.
    SARM1-IN-2
  • HY-P1439
    RS 09
    		Agonist 99.83%
    RS09 is a LPS peptide mimic serves as a candidate to be considered as a new class of TLR4 agonist adjuvant. RS09 increases antibody production in a vaccine setting.
    RS 09
  • HY-103483
    MD2-IN-1
    		Inhibitor 99.89%
    MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD of 189 ?μM for the recombinant human MD2 (rhMD2).
    MD2-IN-1
  • HY-N0774
    Isofraxidin
    		Inhibitor 99.00%
    Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells. Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation.
    Isofraxidin
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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