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-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-W011641
    (±)-Naringenin
    		Inhibitor 99.83%
    (±)-Naringenin is an orally available anti-inflammatory agent that can regulate both acute and chronic inflammation responses, while also showing antioxidant, neuroprotective, liver-protective, and anti-cancer effects. (±)-Naringenin promotes vasodilation in endothelial cells by activating BKCa channels in muscle cells. It also exerts protective effects against experimental colitis by inhibiting Toll-like receptor 4/NF-κB signaling, making it useful in studies related to sepsis, fulminant hepatitis, fibrosis, and cancer research.
    (±)-Naringenin
  • HY-108472
    Loxoribine
    		Agonist 99.94%
    Loxoribine (7-Allyl-8-oxoguanosine) is a guanosine analog with anti-viral and anti-tumor activities. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist.
    Loxoribine
  • HY-113093
    Ethyl glucuronide
    		Agonist 99.22%
    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
  • HY-Y0278
    Chloranil
    		Inducer 98%
    Chloranil (Tetrachloro-p-benzoquinone), an orally active metabolite of pentachlorophenol and hexachlorobenzene, is a widely used fungicide. Chloranil can induce ROS production. Chloranil induces neutrophil extracellular traps through the ROS-JNK-NOX2 pathway. Chloranil induces ferroptosis and neuroinflammation. Chloranil induces apoptosis of mouse embryonic stem cells .
    Chloranil
  • HY-17367A
    Atazanavir sulfate
    		Inhibitor 99.68%
    Atazanavir (BMS-232632) sulfate is a highly selective and orally active HIV-1 protease inhibitor with blood-brain barrier permeability. Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir sulfate inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.
    Atazanavir sulfate
  • HY-135905
    CL264
    		Inhibitor 98.63%
    CL264 is a TLR7-specific agonist for innate immune signals research.
    CL264
  • HY-N1990
    Gypenoside XLIX
    		Inhibitor 99.88%
    Gypenoside XLIX is a multifunctional bioactive compound that can be isolated from Gynostemma pentaphyllum, with a Ka value of 1.58 μM for its binding to SIRT1. Gypenoside XLIX acts as a PPAR-α agonist. It inhibits the activation of TLR4-mediated NF-κB signaling pathway by activating the Sirt1/Nrf2 signaling pathway, reduces ROS accumulation, and alleviates hepatic inflammatory injury in mice with sepsis-induced liver disease. Gypenoside XLIX targets SIRT1 to block YAP-NLRP3 activation and improve sepsis-induced cardiomyopathy. Gypenoside XLIX inhibits apoptosis (Apoptosis), pyroptosis (Pyroptosis), autophagy (Autophagy), lipid peroxidation, pro-inflammatory cytokines and anti-inflammatory cytokines. Gypenoside XLIX alleviates sepsis-induced splenic injury by inhibiting inflammation and oxidative stress, and mitigates sepsis-associated encephalopathy by targeting PPAR-α. Gypenoside XLIX prevents acute kidney injury by inhibiting IGFBP7/IGF1R-mediated programmed cell death and inflammation. Gypenoside XLIX inhibits the expression and activity of vascular cell adhesion molecule-1 in cytokine-induced human endothelial cells. Gypenoside XLIX is applicable to research related to acute liver injury, lung injury, cardiomyopathy, acute splenic injury, sepsis-associated encephalopathy, acute kidney injury, atherosclerosis and chronic inflammation.
    Gypenoside XLIX
  • HY-N2345
    Procyanidin B3
    		Inhibitor 99.92%
    Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis.
    Procyanidin B3
  • HY-W092043
    TLR4-IN-C34-C2-COOH
    		Inhibitor 99.94%
    TLR4-IN-C34-C2-COO is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34-C2-COOH can be used in the research of inflammation and acute myocardial injury. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.
    TLR4-IN-C34-C2-COOH
  • HY-18325
    AN-3485
    		Inhibitor
    AN-3485 is a benzoxaborole analogue and an orally active antagonist of the Toll-like pathway. AN-3485 can inhibit TLR-mediated inflammatory cytokine secretion and has significant anti-inflammatory activity. In addition, AN-3485 also has certain anti-tumor activity.
    AN-3485
  • HY-P11072
    IRF5-CPP5
    		Inhibitor 99.23%
    IRF5-CPP5 is a cytosolic peptide that selectively targeting human IRF5 wirh a Kd of 0.53 μM. IRF5-CPP5 disrupts IRF5 homodimerization and inhibits its nuclear translocation without altering IRF5 phosphorylation levels. IRF5-CPP5 inhibits proinflammatory cytokine (IL-6, IL-1β, TNF-α) production. IRF5-CPP5 can be used for the research of systemic lupus erythematosus.
    IRF5-CPP5
  • HY-117066
    CL075
    		Agonist 99.18%
    CL075 (3M002) is a selective TLR8 agonist with immunomodulating properties. CL075 triggers a MyD88-dependent signaling pathway to elicit production of inflammatory cytokines and type I interferons (IFNs) via activation of NF-κB and IRF7, respectively.
    CL075
  • HY-103698A
    TLR7/8 agonist 1 dihydrochloride
    		Agonist 99.70%
    TLR7/8 agonist 1 dihydrochloride is a toll-like receptor TLR7/TLR8 dual-agonistic imidazoquinoline.
    TLR7/8 agonist 1 dihydrochloride
  • HY-128741
    D-Allose
    		Inhibitor 99.85%
    D-Allose exhibits antitumor activity against various cancer cells. D-Allose scavenges reactive oxygen species (ROS) and reduces oxidative stress damage. D-Allose exhibits anti-inflammatory and neuroprotective through inhibition of TLR4/PI3K/AKT signaling pathway. D-Allose exhibits antihypertensive, cryoprotective, and anti-osteoporotic activities.
    D-Allose
  • HY-150750A
    ODN M362 sodium
    		Agonist
    ODN M362 sodium is a TLR9 agonist that acts as a vaccine adjuvant. ODN M362 sodium activates mouse splenocytes, induces apoptosis in human hepatocellular carcinoma cells, upregulates proinflammatory cytokines in human hepatocellular carcinoma cells, and inhibits the proliferation of human hepatocellular carcinoma cells. ODN M362 sodium upregulates the expression of TLR9/TLR6, activates downstream signaling pathways via IRAK4 and IRF7, and strongly amplifies antigen-specific cellular immune responses to participate in innate immune activation. ODN M362 sodium can be used in research related to hepatocellular carcinoma and breast cancer.
    ODN M362 sodium
  • HY-159069
    Zymosan (ZM), 95%
    		Activator
    Zymosan (ZM), 95% is a yeast cell wall-derived carbohydrate-rich preparation and immunomodulator. Zymosan (ZM), 95% binds to and activates TLR-2, TLR-4, and Dectin-1 receptor to trigger downstream signaling pathways. Zymosan (ZM), 95% upregulates TLR-2, TLR-4, and TNF-α mRNA expression, increases serum TNF-α levels, and stimulates splenocyte number and viability in mice. Zymosan (ZM), 95% attenuates melanoma growth progression, modulates macrophage marker gene expression, and mediates phagocytosis, ROS generation, and cytokine production. Zymosan (ZM), 95% reduces Connexin 43 protein and mRNA levels, inhibits gap junctional intercellular communication, and induces proinflammatory factor production in human corneal cells. Zymosan (ZM), 95% induces peritoneal inflammation in mice, functions as a drug carrier, and supports fibroblast cell attachment in hydrogel formulations. Zymosan (ZM), 95% can be used for the research of melanoma, tumors, fungal keratitis, ocular surface inflammatory disorders, and peritoneal inflammation.
    Zymosan (ZM), 95%
  • HY-13740G
    Resiquimod (GMP)
    		Agonist
    Resiquimod (R848) (GMP) is Resiquimod (HY-13740) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist. Resiquimod (GMP) can induce human mMDSC to mature into inflammatory macrophages.
    Resiquimod (GMP)
  • HY-112050
    CU-CPT-8m
    		Antagonist 99.98%
    CU-CPT-8m is a specific TLR8 antagonist, with an IC50 of 67 nM.
    CU-CPT-8m
  • HY-125390
    SM-360320
    		Agonist 99.41%
    SM-360320 (CL-087) is a potent, orally active TLR7 agonist. SM-360320 is a immuno-modulator and exerts an antitumor effect. SM-360320 can act in synergy with DNA vaccines leading to an enhanced Th1 antibody response. SM-360320 can inhibit HCV replication in hepatocytes via a type I IFN-independent mechanism in addition to its IFN-mediated activity.
    SM-360320
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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