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-B0380S1
    Trimebutine-d5 fumarate
    		Inhibitor
    Trimebutine-d5 fumarate is deuterium labeled Trimebutine fumarate. Trimebutine fumarate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine fumarate inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine fumarate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine fumarate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine fumarate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
    Trimebutine-d<sub>5</sub> fumarate
  • HY-183276
    TLR8 antagonist-2
    		Antagonist
    TLR8 antagonist-2 (Compound 35) is a selective TLR8 antagonist with an IC50 of 0.032 μM against hTLR8. TLR8 antagonist-2 potently inhibits TLR8-dependent NF-κB activity in cells stimulated with TL8-506 (HY-20457). TLR8 antagonist-2 can be used in research related to inflammatory and immune diseases.
    TLR8 antagonist-2
  • HY-150738B
    FITC-labeled ODN 2088 sodium
    		Antagonist
    FITC-labeled ODN 2088 (sodium) is a potent TLR3, TLR7 and TLR9 inhibitor. FITC-labeled ODN 2088 (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 ODN 2088 sodium
  • HY-179275
    TLR7 agonist 33
    		Agonist
    TLR7 agonist 33 (Compound 141) is a potent TLR7 activator with an EC50 of 1 nM. TLR7 agonist 33 can be used for cancer research.
    TLR7 agonist 33
  • HY-145886
    TLR7/8 antagonist 1
    		Antagonist
    TLR7/8 antagonist 1 (Compound 16c) is a competitive TLR7/8 antagonist with IC50 values of 3.91 μM and 2.19 μM, respectively. TLR7/8 antagonist 1 reduces agonist-induced production of proinflammatory cytokines, including TNFα, IFNγ and IL-1β.
    TLR7/8 antagonist 1
  • HY-159918
    AYK005
    		Agonist
    AYK005 is a TLR7/8 immunologic adjuvant.
    AYK005
  • HY-168157
    TLR7 agonist 26
    		Agonist
    TLR7 agonist 26 (Compound 4) is a potent Toll-like receptor 7 (TLR7) agonist, with an EC50 of 225.5 nM. TLR7 agonist 26 shows immunopotentiating effects.
    TLR7 agonist 26
  • HY-159750
    M903
    		Activator
    M903 is a new type of mineral oil-based adjuvant, which belongs to water-in-oil-in-water (w/o/w) emulsion. It can enhance both cellular and humoral immunity against non-specific antigens, stimulate specific immunity against the antigens, delay the release of the antigens in the body, and improve the immunity of animals. It is applicable to various veterinary vaccines, including inactivated vaccines and genetically engineered subunit vaccines, such as pig vaccines for foot-and-mouth disease and blue ear disease.
    M903
  • HY-P2848A
    Cholesterol oxidase, rhodococcus sp
    		Inhibitor
    Cholesterol oxidase, Rhodococcus sp. is a key enzyme in the cholesterol degradation process. It catalyzes the isomerization and oxidation of cholesterol mediated by the coenzyme FAD. Research indicates that cholesterol oxidase plays a crucial role in the pathogenicity of Mycobacterium tuberculosis by modulating the host macrophage immune response through inhibition of the Toll-like receptor 2 (TLR2) signaling pathway, thereby enhancing the survival of Mycobacterium tuberculosis. Cholesterol oxidase, from Rhodococcus sp., shows potential for research in the field of tuberculosis.
    Cholesterol oxidase, rhodococcus sp
  • HY-186062
    HCN-IN-1
    		Inhibitor
    HCN-IN-1 is a TLR4 inhibitor and HCN channel modulator with activity against HCN2 and HCN4.HCN-IN-1 inhibits TLR4-mediated alkaline phosphatase (SEAP) signal activity.HCN-IN-1 reduces HCN2 current across tested voltages, shifts voltage-dependent activation to more hyperpolarized potentials, slows activation kinetics, and does not affect deactivation process.HCN-IN-1 blocks HCN4 current.HCN-IN-1 exhibits analgesic, anti-inflammatory, and anti-anginal effects.HCN-IN-1 can be used for the research of inflammatory pain, neuropathic pain, heart failure, inflammation.
    HCN-IN-1
  • HY-P11093
    Papiliocin
    		Inhibitor
    Papiliocin is a potent peptide antibiotic with both anti-inflammatory and antibacterial activities. Papiliocin is primarily active against Gram-negative bacteria. Papiliocin exhibits strong anti-inflammatory activity against cell, exerting its anti-inflammatory activity by inhibiting the production of NO and the secretion of TNF-α and MIP-2. Papiliocin participates in the innate defense response mechanism by inhibiting the Toll-like receptor pathway and NF-κB. Papiliocin induces apoptosis in fungal cells and increases the total level of intracellular ROS. Papiliocin acts as an effective antiseptic peptide in sepsis models. Papiliocin is useful in anti-inflammatory and antibacterial research.
    Papiliocin
  • HY-117686
    AZ12441970
    		Agonist
    AZ12441970 is a potent and selectiveToll-like receptor 7 (TLR7) agonist, exhibiting pEC50s of 6.8 and 6.6 for human and rat TLR7. AZ12441970 shows efficacy in a mouse allergic airway model with minimal induction of systemic IFN-α. AZ12441970 can be used for allergic airway disease research.
    AZ12441970
  • HY-156175
    TLR7 agonist 14
    		Agonist
    TLR7 agonist 14 (compound 17b) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 14 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations.
    TLR7 agonist 14
  • HY-B0180S1
    Imiquimod-d9
    		Agonist
    Imiquimod-d9 is deuterium labeled Imiquimod. 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-d<sub>9</sub>
  • HY-B0180S
    Imiquimod-d6
    		Agonist
    Imiquimod-d6 is the deuterium labeled Imiquimod. 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-d<sub>6</sub>
  • HY-109137R
    Selgantolimod (Standard)
    		Agonist
    Selgantolimod (Standard) is the analytical standard of Selgantolimod (HY-109137). This product is intended for research and analytical applications. Selgantolimod (GS-9688) is an orally active, potent and selective toll-like receptor 8 (TLR8) agonist for the treatment of hepatitis B virus (HBV) and human immunodeficiency virus (HIV) infection.
    Selgantolimod (Standard)
  • HY-N12378A
    α-Patchoulene
    		Inhibitor
    α-Patchoulene is an orally active anti-inflammatory, antioxidant, and anti-apoptotic agent. α-Patchoulene inhibits the NF-κB, TLR4, and cAMP/PKA/CREB signaling pathways; activates the Sirt1/Nrf2 and AMPK signaling pathways; and targets Fas/FasL, Caspase-3, ERK1/2, ROCK1/MLC2 for inhibition. α-Patchoulene regulates cytokine secretion, inflammatory cell infiltration, lipid peroxidation, cell polarization, gut microbiota, and lipid metabolism, restores barrier function, mitochondrial function, and cell viability, and exhibits repellent activity against Spodoptera exigua larvae. α-Patchoulene can be used in research related to various inflammatory, ischemic, fibrosis-associated diseases, as well as hepatocellular carcinoma.
    α-Patchoulene
  • HY-N7264R
    7α-Hydroxycholesterol (Standard)
    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 (Standard)
  • HY-B0380AR
    Trimebutine maleate (Standard)
    		Inhibitor
    Trimebutine maleate (Standard) is the analytical standard of Trimebutine maleate (HY-B0380A). This product is intended for research and analytical applications. Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
    Trimebutine maleate (Standard)
  • HY-159919
    UM-3006
    		Agonist
    UM-3006 is a highly efficient TLR7/8 agonist that enhances immune responses by activating the TLR signaling pathway. UM-3006 holds significant research and application potential in the fields of vaccine adjuvants and immune diseases.
    UM-3006
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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