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

Toll-like Receptor (TLR) Antagonist

Toll-like Receptor (TLR) Antagonists (23):

Cat. No. Product Name Effect Purity
  • HY-105070A
    Eritoran tetrasodium
    Antagonist
    Eritoran tetrasodium (E5564) is a Toll-like receptor 4 (TLR4) antagonist. Eritoran tetrasodium protects mice against lethal influenza virus infection, such as Ebola virus (EBOV), Marburg virus (MARV). Eritoran tetrasodium decreases the level of granulocytosis, may alleviate the severity of the "cytokine storm". Eritoran tetrasodium inhibits pathogenesis of filovirus infection. Eritoran tetrasodium has anti-inflammatory activity.
  • HY-139567
    Afimetoran
    Antagonist 99.37%
    Afimetoran (BMS-986256) is an orally active, selective, and highly bioavailable TLR7/8 antagonist. Afimetoran (BMS-986256) can inhibit TLR7/8 activation of the NF-κB pathway and reverse TLR7 mediated resistance to steroid induced apoptosis in plasma cell like dendritic cells (pDCs). Afimetoran (BMS-986256) can be used for research on inflammation and autoimmune diseases (systemic lupus erythematosus).
  • HY-116961
    TH1020
    Antagonist 99.81%
    TH1020 is a potent and selective toll-like receptor 5 (TLR5)/flagellin complex antagonist with an IC50 of 0.85 μM. TH1020 inhbits flagellin-induced TLR5 signaling. TH1020 is inactive against TLR2, TLR3, TLR4, TLR7 and TLR8.
  • HY-150751
    ODN TTAGGG
    Antagonist 99.87%
    ODN TTAGGG (A151), inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3'.
  • 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.
  • 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.
  • HY-150738C
    ODN 2088 sodium
    Antagonist
    ODN 2088 sodium is a potent TLR3, TLR7 and TLR9 inhibitor. ODN 2088 sodium shows no cytotoxic. ODN 2088 inhibits the release of IFN-α and IL-6.
  • HY-B0730
    Pamidronate disodium pentahydrate
    Antagonist ≥98.0%
    Pamidronate disodium pentahydrate, the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronate disodium pentahydrate significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of osteoprotegerin in cartilage and subchondral bone, and inhibiting the expression of RANKL and MMP-9 in both tissues, as well as TLR-4 in cartilage, thereby alleviating cartilage degeneration. Additionally, Pamidronate disodium pentahydrate can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma.
  • HY-150751C
    ODN TTAGGG sodium
    Antagonist
    ODN TTAGGG sodium, inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG sodium is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG sodium can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3'.
  • HY-131952
    TLR7/8/9-IN-1
    Antagonist 98.51%
    TLR7/8/9-IN-1 is a potent and orally bioavailable small molecule antagonist (IC50 = 43 nM) of Toll-like receptors 7/8/9 (TLR7/8/9).
  • HY-120538
    CPG-52364
    Antagonist 98.49%
    CPG-52364 (compound 2) is a TLR9 antagonist. CPG-52364 inhibits the HEK293-hTLR9 cell with an IC50 value of 4.6 nM.
  • 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.
  • 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.
  • HY-N0201R
    Atractylenolide I (Standard)
    Antagonist
    Atractylenolide I (Standard) is the analytical standard of Atractylenolide I. This product is intended for research and analytical applications. Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
  • HY-153460
    TLR7/8/9 antagonist 2
    Antagonist
    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.
  • HY-150751B
    FITC-labeled ODN TTAGGG sodium
    Antagonist
    FITC-labeled ODN TTAGGG (sodium), a inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. FITC-labeled ODN TTAGGG (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.
  • HY-B0730R
    Pamidronate disodium pentahydrate (Standard)
    Antagonist
    Pamidronate (disodium pentahydrate) (Standard) is the analytical standard of Pamidronate (disodium pentahydrate). This product is intended for research and analytical applications. Pamidronate disodium pentahydrate, the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronate disodium pentahydrate significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of osteoprotegerin in cartilage and subchondral bone, and inhibiting the expression of RANKL and MMP-9 in both tissues, as well as TLR-4 in cartilage, thereby alleviating cartilage degeneration. Additionally, Pamidronate disodium pentahydrate can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma.
  • HY-P10208
    RKH
    Antagonist
    PKH is a TLR4 antagonist. PKH is a novel tripeptide and can be isolated from Akkermansia muciniphila. RKH reduces sepsis-induced inflammatory cell activation and proinflammatory factor overproduction.
  • 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.
  • HY-145886
    TLR7/8 antagonist 1
    Antagonist
    TLR7/8 Antagonist 1 (Compound 16c) is the potent antagonist of TLR7/8 with IC50s of 3.91 and 2.19 μM, respectively. TLR7/8 Antagonist 1 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for researching infectious disease, cancer, and autoimmune disorders.