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-111792
    GSK1795091
    		Agonist
    GSK1795091 (CRX-601), an immunologic stimulator, is a synthetic TLR4 agonist. Antitumor activity. GSK1795091 can be used as a vaccine adjuvant to enhance both mucosal and systemic immunity to influenza virus vaccines. Not only, GSK1795091 inhibits tumor growth and increases the survival in mice model, but results in long term survival in influenza challenge model in mice.
    GSK1795091
  • HY-144619
    TLR7/8 antagonist 2
    		Antagonist 99.68%
    TLR7/8 antagonist 2 (Compound 15) is a potent and orally active agonist of TLR7/8 with IC50s of 4.9 and 0.6 nM, respectively. Inappropriate activation of TLR7 and TLR8 is linked to several autoimmune diseases, such as lupus erythematosus. TLR7/8 antagonist 2 has the potential for the research of autoimmune diseases.
    TLR7/8 antagonist 2
  • HY-150746
    ODN 24991
    		Inhibitor 99.64%
    ODN 24991, a guanine-modified inhibitory oligonucleotide (INH-ODN), is a TLR3, TLR7 and TLR9 (Toll-like receptor) inhibitor, and its parent is INH-ODN 2088. ODN 24991 disrupts TLR3-, TLR7- and TLR9-mediated immune cell immune responses. ODN 24991 sequence: 5'-C-C-T-G-G-C-c7rGm-G-G-G-3'.
    ODN 24991
  • HY-RS14580
    TLR2 Human Pre-designed siRNA Set A
    		Inhibitor

    TLR2 Human Pre-designed siRNA Set A contains three designed siRNAs for TLR2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    TLR2 Human Pre-designed siRNA Set A
  • HY-178136
    MyD88-IN-3
    		Inhibitor 99.33%
    MyD88-IN-3 is an orally active, selective MyD88 Inhibitor. MyD88-IN-3 specifically targets the TIR domain of MyD88 (KD = 28.5 μM), thereby preventing MyD88 self-polymerization and interaction with TLRs, which suppresses the activation of MAPK and NF-κB pathways. MyD88-IN-3 demonstrates significant anti-inflammatory efficacy and effectively mitigates Acute Lung Injury (ALI) symptoms in CLP (cecal ligation and puncture) and Lipopolysaccharides (HY-D1056) (LPS)-induced ALI models. MyD88-IN-3 can be used for the study of ALI.
    MyD88-IN-3
  • HY-153460
    TLR7/8/9 antagonist 2
    		Antagonist 98.96%
    TLR7/8/9 antagonist 2 is an orally active TLR7/8/9 antagonist. TLR7/8/9 antagonist 2 has inhibitory activities for HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC50 values of 0.011 μM, 0.029 μM and 0,052 μM, respectively.TLR7/8/9 antagonist 2 has high bioavailability in vivo.TLR7/8/9 antagonist 2 can be used for the research of auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis.
    TLR7/8/9 antagonist 2
  • HY-B1900R
    Methylprednisolone succinate (Standard)
    		Inhibitor
    Methylprednisolone succinate (Standard) is the analytical standard of Methylprednisolone succinate (HY-B1900). This product is intended for research and analytical applications. Methylprednisolone succinate (Methylprednisolone hydrogen succinate) is a prodrug of Methylprednisolone (HY-B0260) and glucocorticoid with immunosuppressant and anti-inflammatory activity. Methylprednisolone succinate binds cytosolic glucocorticoid receptors, translocates to nuclei, and modulates target gene transcription. Methylprednisolone succinate alters Bax, Bcl-2, occludin, and ZO-1 expression; attenuates TLR4/NF-κB signaling; suppresses proinflammatory cytokine production and immune cell activation. Methylprednisolone succinate can be used for the research of intracranial haemorrhage, rheumatoid arthritis, multiple sclerosis, preterminal cancer, inflammatory conditions, shock, immediate-type hypersensitivity, acute myocardial ischemia, hypoxic heart muscle damage, and traumatic spinal cord injury.
    Methylprednisolone succinate (Standard)
  • 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-N3097
    Pellitorine
    		Inhibitor 99.84%
    Pellitorine is a bioactive natural amide compound. Pellitorine can competitively antagonize the activation of TRPV1 by Capsaicin (HY-10448), thereby reducing pain signal transmission. Pellitorine improves cognitive dysfunction by upregulating the BDNF-ERK1/2-CREB and Nrf2-HO-1 pathways. Pellitorine exerts anti-inflammatory and anti-sepsis effects by inhibiting the release of high mobility group protein B1 (HMGB1) and the expression of RAGE/TLR4. Pellitorine exerts its antithrombotic effect by prolonging the clotting time, inhibiting the activity of clotting factors and thrombin. Pellitorine inhibits lipid peroxidation and resists ferroptosis by upregulating GPX4 and DHODH. Pellitorine kills Aedes aegypti mosquito larvae by inhibiting V-type H⁺-ATPase and aquaporin 4 (AaAQP4). Pellitorine exhibits anti-cancer activity (e.g., leukemia and breast cancer) and has inhibitory effects on certain bacteria.
    Pellitorine
  • 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-146245B
    FITC-labeled ODN 1826 sodium
    		Agonist
    FITC-labeled ODN 1826 (sodium), a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. FITC-labeled ODN 1826 (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 1826 sodium
  • HY-123789
    T5342126
    		Antagonist 98.1%
    T-5342126 is a toll-like receptor 4 (TLR4) antagonist. It reduces LPS-induced production of nitric oxide (NO) in RAW 264.7 cells (IC50=27.8 μM), as well as decreases LPS-induced IL-8, TNF-α, and IL-6 production in isolated human whole blood (IC50s=110.5, 315.6, and 318.4 μM, respectively). T-5342126 (82 mg/kg) reduces ethanol intake and the abundance of ionized calcium-binding adapter molecule 1 (Iba1), a marker of microglial activation, in the central nucleus of the amygdala in ethanol-dependent mice.
    T5342126
  • HY-158694A
    TLR7 agonist 20 hydrochloride
    		Agonist 99.86%
    TLR7 agonist 20 hydrochloride is a selective Toll-like receptor 7 (TLR7) agonist with an EC50 of 0.22 μM. TLR7 agonist 20 hydrochloride, as an immunostimulant and vaccine adjuvant, enhances the production of anti-spike protein antibodies, increases IgG2b and IgG2c levels, and thereby drives Th1-type immune responses in mice. TLR7 agonist 20 hydrochloride can be used in studies related to non-inflammatory potent vaccine adjuvants.
    TLR7 agonist 20 hydrochloride
  • HY-153839A
    ODN 4084-F sodium
    		Inhibitor
    ODN 4084-F sodium is a class B (‘broadly-active’) inhibitory ODN. ODN 4084-F sodium is potent inhibitor of TLR9-induced B cells and macrophages.
    ODN 4084-F sodium
  • HY-172967
    SARM1-IN-5
    		Inhibitor 99.93%
    SARM1-IN-5 (compound 1-23-a) is a SARM1 inhibitor. SARM1-IN-5 can be used in the study of axonal degeneration related diseases such as Alzheimer’s disease, Parkinson’s disease, amyotrophic lateral sclerosis (ALS), and multiple sclerosis (MS).
    SARM1-IN-5
  • HY-N14039
    Pinus pinaster bark extract
    		Activator
    Pinus pinaster bark extract is extracted from the bark of pine bark with antioxidant, anti-inflammatory and neuroprotective effects. Pinus pinaster bark extract increases toll-like receptor (TLR) activity, inducing production of IL-10.
    Pinus pinaster bark extract
  • HY-144501
    D18
    		Agonist 98.79%
    D18 is an immune modulator. D18 acts as a TLR7/8 dual agonist (EC50 = 24 nM for hTLR7 and 10 nM for hTLR8, respectively). D18 increases PD-L1 expression through epigenetic regulation, thus sensitizing tumors to PD-1/PD-L1 blockade. D18 is a ADC cytotoxin uesd for the systhesis of ADC HE-S2 (HY-144497). D18 has strong immune activation and anti-tumor activity. D18 commonly used in cancer research, such as colon cancer.
    D18
  • HY-N8284
    Tomentosin
    		Inhibitor 98.95%
    Tomentosin is an orally active natural sesquiterpenoid lactone. Tomentosin exhibits multiple activities such as anti-tumor, anti-fungal, anti-inflammatory, anti-oxidant and neuroprotective effects. Tomentosin can inhibit tumor cell proliferation, migration and invasion, and induce apoptosis. Tomentosin can be used in the research of tumors, inflammation and nervous system diseases.
    Tomentosin
  • HY-113093S
    Ethyl glucuronide-d5
    		Agonist
    Ethyl glucuronide-d5 is the deuterium labeled Ethyl glucuronide (HY-113093). Ethyl glucuronide is an endogenous metabolite. Ethyl glucuronide is the metabolite of ethanol. Ethyl glucuronide is a biomarker for ethanol exposure that accumulates in hair and reflects the alcohol intake over a time period. Ethyl glucuronide is the agonist for TLR4.
    Ethyl glucuronide-d<sub>5</sub>
  • HY-153838A
    ODN 5328 sodium
    		Inhibitor
    ODN 5328 (ODN 2395 Control) sodium can be used as a sequence control for C-class ODN 2395. ODN 5328 sodium shares the sequence with ODN 2395 but contain GpC dinucleotides instead of the CpG motifs.
    ODN 5328 sodium
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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