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-134581A
    Enpatoran hydrochloride
    		Inhibitor 99.42%
    Enpatoran (M5049) hydrochloride is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran hydrochloride is inactive against TLR3, TLR4 and TLR9. Enpatoran hydrochloride can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran hydrochloride exhibits excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be used for both innate and adaptive autoimmunity blocking research.
    Enpatoran hydrochloride
  • HY-139413
    β-D-Glucan
    		99.00%
    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-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-150741
    ODN 2216
    		Agonist
    ODN 2216 is a human-specific TLR9 (toll-like receptor 9) ligand or agonist. ODN 2216 induces high amounts of IFN-α and IFN-β. ODN 2216 induces IFN-α by pDC (plasmacytoid DC) and IL-12 (p40) production by DC (dendritic cells). ODN 2216 stimulates IFN-γ production in peripheral blood mononuclear cells (PBMC), which is indirect and mediated by IFN-α/β. ODN 2216 can activate NK cells and promote IFN-γ production of TCR-triggered CD4+ T cells.
    ODN 2216
  • HY-109137
    Selgantolimod
    		Agonist 98.18%
    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
  • HY-150724
    ODN 1018
    		Agonist 99.28%
    ODN 1018 (1018 ISS), an oligodeoxynucleotide, is a TLR-9 agonist. ODN 1018 is also a synthetic immunostimulatory sequence that can be used as vaccine adjuvant. Sequence: 5′-TGACTGTGAACGTTCGAGATGA-3′.
    ODN 1018
  • HY-150743C
    ODN 2395 sodium
    		Agonist 98.20%
    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-W145499
    Zinc Gluconate
    		Inhibitor 98.2%
    Zinc Gluconate is a zinc supplement in the form of a gluconate salt, which plays a role in various physiological processes such as immune function, wound healing, and olfaction. Zinc Gluconate has a LD50 of 39.6 mg/kg in mice (Tail vein injection). Zinc Gluconate can be used in the research of inflammation, zinc deficiency, colds, cancer, and nutritional supplements.
    Zinc Gluconate
  • HY-134816
    D-Glucan
    		Activator
    D-Glucan is an orally effective Dectin-1 receptor immune activator with antioxidant properties (reducing TNF-α). D-Glucan activates macrophages and neutrophils to scavenge free radicals, inhibit oxidative stress and inflammatory responses, and improve insulin sensitivity. D-Glucan promotes glycolysis by enhancing the activity of the antioxidant enzyme glutathione, inhibiting gluconeogenesis and activating GK. D-Glucan can be used in the research of liver damage protection (antagonizing Acetaminophen (HY-66005) toxicity), radiation protection (synergistic with vitamin E) and diabetes (improving glucose metabolism).
    D-Glucan
  • HY-148045
    TLR9-IN-1
    		Inhibitor 99.67%
    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-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-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.
    RS 09
  • HY-17003
    Saquinavir mesylate
    		Inhibitor 99.84%
    Saquinavir (Ro 31-8959) mesylate is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir mesylate also has anti-inflammatory activity and can induce apoptosis of human red blood cells.
    Saquinavir mesylate
  • HY-U00435
    Neoseptin 3
    		Agonist 99.21%
    Neoseptin 3 is a Toll-like receptor 4/myeloid differentiation factor 2 (mTLR4/MD-2) agonist with an EC50 of 18.5 μM.
    Neoseptin 3
  • HY-D1056B3
    Lipopolysaccharides, from Klebsiella pneumoniae
    		Activator
    Lipopolysaccharides, from Klebsiella pneumoniae (LPS, from bacterial (Klebsiella pneumoniae)) are lipopolysaccharide endotoxins and TLR4 activators derived from Klebsiella pneumoniae, and are classified as S-type LPS. Lipopolysaccharides, from Klebsiella pneumoniae exhibit a typical three-part structure: O-antigen, core oligosaccharide, and lipid A. Lipopolysaccharides, from Klebsiella pneumoniae may participate in bacterial immune evasion by inhibiting complement-mediated killing and suppressing the host's secretion of antimicrobial peptides, thereby allowing the bacteria to escape immune defenses. Lipopolysaccharides, from Klebsiella pneumoniae possess high viscosity and resistance to serum-mediated killing, which may lead to sepsis. Lipopolysaccharides, from Klebsiella pneumoniae can be used to construct animal models of sepsis.
    It is recommended to prepare a stock solution of ≥2 mg/mL and ensure that it is fully mixed and dissolved. Due to the adsorption characteristics of LPS, low adsorption centrifuge tubes should be used for aliquoting and storage.
    Lipopolysaccharides, from Klebsiella pneumoniae
  • 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 for human health prevention, and its derivatives also possess anti-tumor activity.
    D-Glucuronic acid
  • HY-17367
    Atazanavir
    		Inhibitor 99.86%
    Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.
    Atazanavir
  • 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-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-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.
    Teneligliptin hydrobromide hydrate
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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