1. Signaling Pathways
  2. Immunology/Inflammation
  3. Toll-like Receptor (TLR)

Toll-like Receptor (TLR)

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N7264
    7α-Hydroxycholesterol
    99.99%
    7α-Hydroxycholesterol is a cholesterol oxide and can serve as a biomarker for oxidative stress and lipid peroxidation. 7α-Hydroxycholesterol has cytotoxic and pro-inflammatory activities. 7α-Hydroxycholesterol can also inhibit sterol synthesis and reduce the activity of HMG-CoA reductase. 7α-Hydroxycholesterol can be used in the research of diseases such as diabetes and atherosclerosis.
    7α-Hydroxycholesterol
  • HY-N0795
    Procyanidin B1
    Antagonist 99.56%
    Procyanidin B1 is a polyphenolic flavonoid isolated from commonly eaten fruits, binds to TLR4/MD-2 complex, and has anti-inflammatory activity.
    Procyanidin B1
  • HY-N6949
    Juglone
    Inhibitor 99.77%
    Juglone (5-hydroxy-1,4-naphthalenedione) is a yellow dye that can be extracted from Juglans regia. Juglone induces apoptosis through the mitochondrial pathway. Juglone has antibacterial and antitumor activity .
    Juglone
  • HY-150743C
    ODN 2395 sodium
    Agonist
    ODN 2395 sodium is a C class oligodeoxynucleotide and can be used as vaccine adjuvant. ODN 2395 sodium is also a TLR9 agonist. Sequence: 5'-tcgtcgttttcggcgc:gcgccg-3'.
    ODN 2395 sodium
  • HY-128799
    CL097
    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
  • 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-P2036A
    FSL-1 TFA
    Agonist 99.65%
    FSL-1 TFA, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection. FSL-1 TFA induces MMP-9 production through TLR2 and NF-κB/AP-1 signaling pathways in monocytic THP-1 cells.
    FSL-1 TFA
  • HY-116213
    Sparstolonin B
    Antagonist 99.94%
    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-150726C
    ODN 1668 sodium
    Agonist
    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-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-D1056A1
    Lipopolysaccharides, from E. coli O111:B4
    Lipopolysaccharides, from E. coli O111:B4 (LPS, from Escherichia coli (O111:B4)) are endotoxins and TLR4 activators extracted from Escherichia coli (E. coli O111:B4) and are classified as S (smooth) type LPS. Lipopolysaccharides, from E. coli O111:B4 possess the typical three-part structure: O-antigen, R3-type core oligosaccharide, and lipid A. Lipopolysaccharides, from E. coli O111:B4 activate TLR-4 in immune cells and can cause significant gastric diseases. Lipopolysaccharides, from E. coli O111:B4 can be used to induce cellular inflammation and establish animal models related to inflammation.
    Lipopolysaccharides, from E. coli O111:B4
  • 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-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-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-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-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-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-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-117066
    CL075
    Agonist 99.25%
    CL075 (3M002) is a selective TLR8 agonist with immunomodulating properties. CL075 triggers a MyD88-dependent signaling pathway to elicit production of inflammatory cytokines and type I interferons (IFNs) via activation of NF-κB and IRF7, respectively.
    CL075
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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