2. Signaling Pathways
  3. Immunology/Inflammation
  4. Toll-like Receptor (TLR)
  5. TLR4 Isoform

TLR4

 
Cat. No. Product Name Effect Purity
  • HY-D1056
    Lipopolysaccharides, from E. coli O55:B5
    		Activator
    Lipopolysaccharides, from E. coli O55:B5 (LPS, from Escherichia coli (O55:B5)) are endotoxins and TLR4 activators extracted from Escherichia coli (E. coli O55:B5) and are classified as S (smooth) type LPS. Lipopolysaccharides, from E. coli O55:B5 possess the typical three-part structure: O-antigen, core oligosaccharide, and lipid A. Lipopolysaccharides, from E. coli O55:B5 activate TLR-4 in immune cells, exhibit high pyrogenicity, and demonstrate dose and serotype specificity. Lipopolysaccharides, from E. coli O55:B5 can be widely used to induce cellular inflammation and establish animal models related to inflammation.
    It is recommended to prepare a solution with concentration ≥2 mg/mL. Vortex thoroughly for more than 10 minutes. Due to the adsorption characteristics of LPS, silanized container or low adsorption centrifuge tubes should be used for aliquoting and storage, and mix thoroughly before use.
  • HY-11109
    Resatorvid
    		Inhibitor 99.95%
    Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. Resatorvid inhibits NO, TNF-α and IL-6 production with IC50s of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy and plays pivotal role in various inflammatory diseases.
  • HY-108910
    Chymotrypsin
    		Inhibitor
    Chymotrypsin (EC 3.4.21.1; Chymotrypsin A) is an orally effective inhibitor targeting molecules such as TLR4, NF-κB, MMP-1, TNF-α, IL-1β, and IL-6. Chymotrypsin downregulates the TLR4/NF-κB signaling pathway, inhibiting the release of inflammatory factors, reducing cell infiltration and tissue damage. It also reduces the expression of tumor cell adhesion molecules (such as CD44 and CD54) and can be specifically detected by fluorescent probes (such as NBD-3). Chymotrypsin has anti-inflammatory, hepatoprotective, joint damage-reducing, liver protection against lipotoxicity, and anti-tumor metastasis functions. It can be used in research on diseases such as rheumatoid arthritis, non-alcoholic fatty liver disease, and melanoma metastasis. Chymotrypsin can be used in studies of inflammation, edema, and expectoration.
  • HY-N0680
    Thiamine hydrochloride
    		Inhibitor 99.97%
    Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.Thiamine hydrochloride activates NrF-2/HO-1 and inhibits TLR4, NF-κB. Thiamine hydrochloride has neuroprotective and anti-inflammatory effects. Thiamine hydrochloride can be used in the studys of diabetic complications, neurological diseases, cancers, and colitis.
  • HY-107575
    TLR4-IN-C34
    		Inhibitor 99.94%
    TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis.
  • HY-W012837
    Benzylmethyl ether
    		98.70%
    Benzylmethyl ether is a derivative of HY-B0892 (Benzyl alcohol). Benzylmethyl ether is an aromatic alcohol, a colorless liquid with a mild aromatic odor. Benzylmethyl ether is an inhibitor of P450 enzyme. Benzylmethyl ether mediated Toll-Like Receptor 4 to reduce the inflammatory response of liver injury in mice.
  • HY-179474
    TSI-13-57
    		Inhibitor 98.73%
    TSI-13-57 is a pan-TLR inhibitor (IC50: 2.7 μM, 6.03 μM, 7.37 μM, 6.38 μM for TLR9, TLR7, TLR2, TLR4, respectively). TSI-13-57 inhibits homodimerization of the TIR domains of MyD88. TSI-13-57 reduces systemic inflammatory responses in LPS-induced mice.
  • HY-179646
    CIAC101
    		Antagonist
    CIAC101 is a potent and brain-penetrant TLR4 antagonist with an IC50 of 17.0 nM in NO assay. CIAC101 blocks Lipopolysaccharides (HY-D1056) (LPS)-induced NF-κB activation and reduces the expression of pro-inflammatory mediators (iNOS, IL-1β, TNF-α, and IL-6). CIAC101 robust antineuroinflammatory activity with efficacy against drug-evoked neurobehavioral adaptations. CIAC101 can be used for the research of addiction and neurological disease.
  • HY-N0703
    Schaftoside
    		Inhibitor 99.70%
    Schaftoside is a flavonoid found in a variety of Chinese herbal medicines, such as Eleusine indica. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission.
  • HY-P1439
    RS 09
    		Agonist 99.88%
    RS 09 is an LPS (HY-D1056) peptide mimic and TLR4 agonist. RS 09 can bind to TLR-4 and activate NF-κB. RS 09 can function as an adjuvant in vivo, enhancing the antigen-specific immune response.
  • 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.
  • HY-N0108
    Physcion
    		Inhibitor 99.40%
    Physcion (Parietin), an anthraquinone derivative derived from the traditional Chinese medicine rhubarb, is an effective oral active 6-phosphogluconate dehydrogenase inhibitor with blood-brain barrier permeability, with IC50 and Kd values of 38.5 μM and 26.0 μM, respectively. Additionally, Physcion is an inhibitor of the <>bTLR4/NF-κB signaling pathway, exhibiting anti-inflammatory, antibacterial, and anticancer effects, and can induce Apoptosis and Autophagy in cancer cells.
  • 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.
  • HY-N6612
    D-Glucuronic acid
    		Agonist 98.0%
    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, and its derivatives also possess anti-tumor activity.
  • 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.
  • HY-N1346
    Robinin
    		Inhibitor 99.96%
    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.
  • HY-14806B
    Teneligliptin hydrobromide hydrate
    		Inhibitor 99.97%
    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.
  • HY-130320
    Monophosphoryl lipid A
    		Agonist 99.87%
    Monophosphoryl lipid A (Glucopyranosyl lipid A) is a toll-like receptor 4 agonist. Monophosphoryl lipid A is derived from the cell wall of nonpathogenic Salmonella. Monophosphoryl lipid A can be used for the research of immunization and vaccine.
  • HY-N0774
    Isofraxidin
    		Inhibitor 99.94%
    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.
  • HY-N7700A
    Guluronic acid sodium
    		Inhibitor 98.0%
    Guluronic acid (G2013) sodium is an orally active oxidative stress regulator and anti-inflammatory agent that exerts pharmacological effects by down-regulating various pro-inflammatory and oxidative stress-related genes (such as TLR4, NF-κB, iNOS, etc.) and inhibiting the activities of COX-2, MMPs and VEGF. Low-dose Guluronic acid sodium up-regulates the expression of immunoregulatory genes SHIP1 and SOCS1, thereby effectively inhibiting cancer-related inflammation, tumor angiogenesis, cell adhesion and metastasis, while reducing the accumulation of immunosuppressive cells. Guluronic acid sodium significantly prolongs the survival time of tumor-bearing hosts within a concentration range without direct cytotoxicity, demonstrating favorable safety. Guluronic acid sodium has involved in the research of multiple sclerosis, ankylosing spondylitis, breast cancer and other inflammatory diseases.
Cat. No. Product Name / Synonyms Species Source