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

Toll-like Receptor (TLR)

(TLR)

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-159750
    M903
    Activator
    M903 is a vaccine adjuvant and a key component in vaccines. Adjuvants can be divided into immunostimulants and delivery systems. Adjuvants can not only enhance the intensity and durability of immune responses, but also affect the type of immune responses. On the one hand, immunostimulants promote the production of antigen signals and co-stimulatory signals by targeting Toll-like receptors (TLRs) and other pattern recognition receptors (PRRs), leading to the maturation and activation of antigen presenting cells (APCs), thereby enhancing adaptive immune responses; on the other hand, delivery systems are carrier materials that promote antigen delivery by prolonging the bioavailability of loaded antigens and targeting antigens to lymph nodes or APCs. Several common adjuvants include: saponins, TLRs agonists, polysaccharides, nanoparticles, cytokines, and mucosal adjuvants.
    M903
  • HY-P2848A
    Cholesterol oxidase, rhodococcus sp
    Inhibitor
    Cholesterol oxidase, Rhodococcus sp. is a key enzyme in the cholesterol degradation process. It catalyzes the isomerization and oxidation of cholesterol mediated by the coenzyme FAD. Research indicates that cholesterol oxidase plays a crucial role in the pathogenicity of Mycobacterium tuberculosis by modulating the host macrophage immune response through inhibition of the Toll-like receptor 2 (TLR2) signaling pathway, thereby enhancing the survival of Mycobacterium tuberculosis. Cholesterol oxidase, from Rhodococcus sp., shows potential for research in the field of tuberculosis.
    Cholesterol oxidase, rhodococcus sp
  • HY-130320A
    Monophosphoryl lipid A free acid
    Agonist
    Monophosphoryl lipid A (free acid) is a toll-like receptor 4 agonist. Monophosphoryl lipid A (free acid) is derived from the cell wall of nonpathogenic Salmonella. Monophosphoryl lipid A (free acid) can be used for the research of immunization and vaccine.
    Monophosphoryl lipid A free acid
  • HY-156175
    TLR7 agonist 14
    Agonist
    TLR7 agonist 14 (compound 17b) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 14 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations.
    TLR7 agonist 14
  • HY-B0180S1
    Imiquimod-d9
    Agonist
    Imiquimod-d9 is deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].
    Imiquimod-d<sub>9</sub>
  • HY-B0180S
    Imiquimod-d6
    Agonist
    Imiquimod-d6 is the deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].
    Imiquimod-d<sub>6</sub>
  • HY-B0380AR
    Trimebutine maleate (Standard)
    Inhibitor
    Trimebutine maleate (Standard) is the analytical standard of Trimebutine maleate (HY-B0380A). This product is intended for research and analytical applications. Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS).
    Trimebutine maleate (Standard)
  • HY-159919
    UM-3006
    Agonist
    UM-3006 is a highly efficient TLR7/8 agonist that enhances immune responses by activating the TLR signaling pathway. UM-3006 holds significant research and application potential in the fields of vaccine adjuvants and immune diseases.
    UM-3006
  • HY-W008341
    5-Chloroisoquinoline
    Inhibitor
    5-Chloroisoquinoline (compound 42) is an inhibitor of SARM1 (Sterile alpha and toll/interleukin receptor (TIR) motif containing protein 1), an enzyme involved in axon degeneration that catalyzes multiple activities through a ternary complex mechanism. 5-Chloroisoquinoline can be used in the study of neurodegenerative diseases or axon degeneration.
    5-Chloroisoquinoline
  • HY-164485
    INI-4001
    Activator
    INI-4001 is a TLR7/8 agonist, with EC50 values of 1.89 μM and 4.86 μM for TLR7/8, respectively. INI-4001 induces signaling and SEAP production through TLR7 and TLR8.
    INI-4001
  • HY-17007R
    Saquinavir (Standard)
    Inhibitor
    Saquinavir (Standard) (Ro 31-8959 (Standard)) is the analytical standard of Saquinavir (HY-17007). This product is intended for research and analytical applications. Saquinavir (Ro 31-8959) is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir also has anti-inflammatory activity and can induce apoptosis of human red blood cells.
    Saquinavir (Standard)
  • HY-173388
    TLR4-IN-2
    Inhibitor
    TLR4-IN-2 (Compound Racemic-11k) is inhibitors of TLR4, JNK, and NF-κB. TLR4-IN-2 inhibits NO production in LPS-stimulated RAW264.7 cells with an IC50 value of 23.2 µM. TLR4-IN-2 exerts anti-inflammatory activity by inhibiting TLR4 expression, reducing JNK phosphorylation, thereby suppressing the activation of NF-κB, blocking the transcription of inflammation-related genes, reducing the expression of iNOS and COX-2, and decreasing the production of inflammatory mediators such as NO, PGE 2, and TNF-α. TLR4-IN-2 is promising for research of inflammatory diseases, such as rheumatoid arthritis and various inflammatory disorders.
    TLR4-IN-2
  • HY-N0022R
    Isoacteoside (Standard)
    Inhibitor
    Isoacteoside (Standard) is the analytical standard of Isoacteoside. This product is intended for research and analytical applications. Isoacteoside is a natural product that can significantly inhibit the formation of glycation end products. Isoacteoside Standard regulates the AKT/PI3K/m-TOR/NF-κB signaling pathway, induces apoptosis in OVCAR-3 cell. Isoacteoside Standard exhibits antitumor, anti-inflammatory, anti-obesity and neuroprotective activities.
    Isoacteoside (Standard)
  • HY-W014223R
    2,4′-Dihydroxybenzophenone (Standard)
    2,4′-Dihydroxybenzophenone (Standard) is the analytical standard of 2,4′-Dihydroxybenzophenone. This product is intended for research and analytical applications. 2,4′-Dihydroxybenzophenone (Ultraviolet absorber UV-0) occupies the hydrophobic pocket of MD2 and blocks the dimerization of TLR4. 2,4′-Dihydroxybenzophenone inhibits the LPS induced mtROS production, and LPS induced inflammatory response by downregulating pro-inflammatory mediators and decreasing the expression of MyD88, p-IRAK4, and NF-κB. 2,4′-Dihydroxybenzophenone is also a UV absorber.
    2,4′-Dihydroxybenzophenone (Standard)
  • HY-N0795R
    Procyanidin B1 (Standard)
    Antagonist
    Procyanidin B1 (Standard) is the analytical standard of Procyanidin B1. This product is intended for research and analytical applications. Procyanidin B1 is a polyphenolic flavonoid isolated from commonly eaten fruits, binds to TLR4/MD-2 complex, and has anti-inflammatory activity.
    Procyanidin B1 (Standard)
  • HY-13655A
    Isatoribine
    Agonist
    Isatoribine is a TLR7 agonist. Isatoribine is used in the study of chronic hepatitis C virus (HCV) infection.
    Isatoribine
  • HY-103697AR
    Gardiquimod diTFA (Standard)
    Gardiquimod (diTFA) (Standard) is the analytical standard of Gardiquimod (diTFA). This product is intended for research and analytical applications. Gardiquimod diTFA is an imidazoline TLR7/8 agonist. Gardiquimod diTFA inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 at concentrations below 10 μM.
    Gardiquimod diTFA (Standard)
  • HY-159914
    AYK004-B1
    Agonist
    AYK004-B1 is a TLR7 agonist (EC50=0.2265 nM). AYK004-B1 can be used to prepare immune adjuvants.
    AYK004-B1
  • HY-103697R
    Gardiquimod (Standard)
    Gardiquimod (Standard) is the analytical standard of Gardiquimod. This product is intended for research and analytical applications. Gardiquimod is an imidazoline TLR7/8 agonist. Gardiquimod inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 at concentrations below 10 μM.
    Gardiquimod (Standard)
  • HY-W130878
    4-Octylphenol
    4-Octylphenol is a hormone disruptor that has gender-specific effects on male reproductive cells, significantly reducing the mitotic index and the number of spermatogonia. 4-Octylphenol can cause inflammatory damage to fish gills by activating the complement system through the C3a/C3aR axis and the C5a/C5aR1 axis, this leads to complement activation and causes immune suppression due to the imbalance between Th1/Th2 cells and regulatory T cells (Treg)/Th17 cells, as well as inflammatory damage via the Toll-like receptor 7 (Toll-like Receptor (TLR))/IκBα/NF-κB pathway.
    4-Octylphenol
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

TLR3

TLR8

TLR9

TLR2

TLR4

TLR7

TLR1

TLR6

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Toll-like Receptor (TLR) Ligands, Inducers, Inhibitors, Agonists, Antagonists, Activators & Modulators
Product NameTLR3TLR8TLR9TLR2TLR4TLR7TLR1TLR6Purity    
Lipopolysaccharides, from E. coli O55:B5    
TLR4
   
Resiquimod 
TLR8
   
TLR7
  99.95%
Resatorvid    
TLR4
   99.95%
TLR4/NF-κB-IN-1    
TLR4
   
Imiquimod     
TLR7
  99.96%
C29   
TLR2
    ≥98.0%
Pam3CSK4 TFA   
TLR2
  
TLR1
 99.66%
Hydroxychloroquine sulfate  
TLR9
  
TLR7
  99.99%
CU-CPT 4a
TLR3, IC50: 3.44 μM (in RAW 264.7 cells)
       99.34%
Agatolimod sodium  
TLR9
     98.49%
ODN 1826 sodium  
TLR9
     99.51%
Enpatoran 
TLR8, IC50: 24.1 nM (in HEK293 cells)
TLR8, IC50: 620 nM (in peripheral blood mononuclear cells (PBMCs))
TLR8, IC50: 120 nM ( in whole blood (WB) cells)
   
TLR7, IC50: 11.1 nM (in HEK293 cells)
TLR7, IC50: 68.3 nM (in peripheral blood mononuclear cells (PBMCs))
TLR7, IC50: 2.2 nM ( in whole blood (WB) cells)
  99.80%
Polyinosinic-polycytidylic acid sodium
TLR3
       99.40%
ODN 1826  
TLR9
     
CU-CPT22   
TLR2
  
TLR1
 ≥99.0%
Diprovocim   
TLR2
  
TLR1
 98.82%
Imiquimod hydrochloride     
TLR7
  99.77%
TLR4-IN-C34    
TLR4
   99.90%
Agatolimod  
TLR9
     98.32%
Motolimod 
TLR8
      98.12%
Telratolimod 
TLR8
   
TLR7
  98.85%
Thiamine hydrochloride    
TLR4
   99.97%
Atractylenolide I  
TLR9
  
TLR7
  99.94%
Vesatolimod     
TLR7
  99.90%
Physcion    
TLR4
   99.10%
Schaftoside    
TLR4
   99.67%
AT791  
TLR9, IC50: 0.04 μM
  
TLR7, IC50: 3.33 μM
  98.77%
MMG-11   
TLR2
    99.24%
ODN 2216  
TLR9
     
CU-T12-9   
TLR2, EC50: 52.9 nM (in HEK-Blue cells)
  
TLR1, EC50: 52.9 nM (in HEK-Blue cells)
 99.96%
Enpatoran hydrochloride 
TLR8, IC50: 24.1 nM
   
TLR7, IC50: 11.1 nM
  99.42%
ODN 1018  
TLR9
     
Selgantolimod 
TLR8
      98.18%
ODN 2395  
TLR9
     98.39%
ODN 1668 sodium  
TLR9
     98.79%
ODN 2395 sodium  
TLR9
     98.20%
Neoseptin 3    
TLR4, EC50: 18.5 μM
   99.21%
CL097 
TLR8
   
TLR7
  99.90%
Sparstolonin B   
TLR2
TLR4
   99.94%
TLR9-IN-1  
human TLR9, IC50: 7 nM
     99.67%
Okanin    
TLR4
   99.98%
FSL-1 TFA   
TLR2
   
TLR6
99.65%
Gardiquimod 
TLR8
   
TLR7
  99.91%
D-Glucuronic acid    
TLR4
   
RS 09    
TLR4
   99.88%
TLR7/8-IN-1 
TLR8
   
TLR7
  99.92%
CL075 
TLR8
      99.18%
RS 09 TFA    
TLR4
   99.81%
Teneligliptin hydrobromide hydrate    
TLR4
   99.87%
ODN 1668  
TLR9
     98.79%
ssRNA40 sodium 
TLR8
   
TLR7
  
IAXO-102    
TLR4
   ≥98.0%
E6446 dihydrochloride  
TLR9
  
TLR7
  99.96%
TLR7/8 agonist 1 
TLR8
   
TLR7
  98.42%
Robinin   
TLR2
TLR4
   99.09%
MD2-IN-1    
TLR4
   99.89%
Isofraxidin    
TLR4
   99.93%
Loxoribine     
TLR7
  99.66%
CU-CPT-9a 
TLR8, IC50: 0.5 nM
      99.74%
Dracorhodin perchlorate    
TLR4
   99.14%
Gardiquimod diTFA 
TLR8
   
TLR7
  ≥99.0%
TL8-506 
TLR8, EC50: 30 nM
      
NecroX-7    
TLR4
   99.69%
Monophosphoryl lipid A    
TLR4
   ≥99.0%
CAY10614    
TLR4, IC50: 1.675 μM (in HEK293 cells)
   98.87%
TLR7/8 agonist 3 
TLR8
   
TLR7
  99.96%
DSR-6434     
TLR7, EC50: 7.2 nM (Human)
TLR7, EC50: 4.6 nM (Mice)
  99.32%
CL264     
TLR7
  98.63%
AN-3485
TLR3
  
TLR2
TLR4
   
CU-CPT-8m 
TLR8, IC50: 67 nM
      99.98%
AXC-715 trihydrochloride 
TLR8, EC50: 1.6 μM
   
human TLR7, EC50: 0.643 μM
  99.76%
L6H21    
TLR4
   99.19%
L48H37    
TLR4
   
CU-CPT17e
TLR3
TLR8
TLR9
     99.00%
Procyanidin B3    
TLR4
   99.92%
Kaempferol 3-O-sophoroside   
TLR2
TLR4
   99.41%
CpG ODN 10101  
TLR9
     
ODN M362  
TLR9
     
E6446  
TLR9
  
TLR7
  ≥98.0%
MD2-TLR4-IN-1    
TLR4
   99.62%
Imiquimod maleate     
TLR7
  99.25%
TLR7 agonist 3     
TLR7
  99.90%
CU-115 
TLR8, IC50: 1.04 μM
   
TLR7, IC50: 50 μM
  99.55%
ODN 20844  
TLR9
  
TLR7
  
Chloranil    
TLR4
   98%
GSK2245035     
TLR7
  99.85%
RKH acetate    
TLR4
   99.45%
C12-TLRa 
TLR8
   
TLR7
  ≥99.0%
Magnesium citrate    
TLR4
   ≥98.0%
Fosfenopril    
TLR4
   99.89%
CU-CPT9b 
TLR8, IC50: 0.7 nM
TLR8, Kd: 21 nM
      99.03%
Resiquimod (GMP) 
TLR8
   
TLR7
  
AZD8848     
TLR7
  99.14%
Hydroxychloroquine (sulfate) (Standard)  
TLR9
  
TLR7
  99.28%
Polygalasaponin F    
TLR4
   99.85%
MAPK-IN-1    
TLR4
   
PF-4878691     
TLR7
  99.89%
1V209     
TLR7
  99.67%
TLR7/8 agonist 4 
TLR8
   
TLR7
  99.04%
SM-324405     
human TLR7, pEC50: 7.3
Rat TLR7, pEC50: 6.6
TLR7, EC50: 50 nM
  98.52%
LHC-165     
TLR7
  ≥98.0%
CL097 hydrochloride 
TLR8
   
TLR7
  99.90%
E104     
TLR7
  
BBIQ     
TLR7, EC50: 59.1 nM (Human TLR7)
  99.85%
TLR7 agonist 1     
TLR7, IC50: 90 nM
  98.19%
MMG-11 quarterhydrate   
TLR2
    98.70%
TLR7 agonist 6     
TLR7, EC50: ~4 nM
  98.08%
FAM-labeled ODN 1826 sodium  
TLR9
     98.03%
Resiquimod-d5 
TLR8
   
TLR7
  99.84%
Kdo2-Lipid A ammonium    
TLR4
   99.00%
ORN 06 sodium     
TLR7
  
SMU-L11     
TLR7, EC50: 0.024 μM
  99.64%
PVP-037.2 
TLR8
   
TLR7
  99.18%
TMX-201     
TLR7
  
ODN M326 sodium  
TLR9
     
MC-Val-Cit-PAB-Amide-TLR7 agonist 4 
TLR8
   
TLR7
  99.39%
TLR7 agonist 4     
TLR7, EC50: 4.3 nM
  98.87%
AXC-715 hydrochloride 
TLR8, EC50: 1.6 μM
   
TLR7, EC50: 0.643 μM
  99.46%
TLR4-IN-C34-C2-amide-C6-OH    
TLR4
   99.62%
ODN 24987  
TLR9
     
Pam3CSK4   
TLR2
  
TLR1
 
TLR7 agonist 20 hydrochloride 
TLR8, EC50: 17.21 μM
   
TLR7, EC50: 0.23 μM
  99.86%
Tomentosin   
TLR2
TLR4
   98.95%
ODN 24888  
TLR9
  
TLR7
  
TLR7/8 agonist 8 
TLR8, EC50: 12 nM
   
TLR7, EC50: 27 nM
  98.69%
Diprovocim-X   
TLR2
  
TLR1
 98.64%
MTvkPABC-P5 TFA     
TLR7
  98.78%
(S)-Hydroxychloroquine  
TLR9
  
TLR7
  
Guretolimod     
TLR7
  
(R)-Hydroxychloroquine  
TLR9
  
TLR7
  
TLR8 agonist 2 hydrochloride 
TLR8, EC50: 3 nM
   
TLR7, EC50: 33.33 μM
  
TLR8 agonist 2 
TLR8, EC50: 3 nM
   
TLR7, EC50: 33.33 μM
  
TLR7/8 agonist 4 TFA 
TLR8
   
TLR7
  
UC-1V150     
TLR7
  
SjDX5-271    
TLR4
   
Mumefural    
TLR4
   
TLR7 agonist 17     
human TLR7, EC50: 12 nM
mTLR7, EC50: 17 nM
  
ORN 06     
TLR7
  
WYJ-2   
TLR2
    
TLR7 agonist 20 
TLR8, EC50: 17.21 μM
   
TLR7, EC50: 0.23 μM
  
TLR7-IN-1     
TLR7, IC50: 0.001 μM
  
TLR7 agonist 28     
TLR7
  
Tri(TLR4-IN-C34-C2-amide-C3-amide-PEG1)-amide-C3-COOH    
TLR4
   
TLR7 agonist 29     
human TLR7, EC50: 5.2 nM
mTLR7, EC50: 48.2 nM
  
BI1543673 
TLR8
  
TLR4
TLR7
  
TLR7 agonist 7     
TLR7, EC50: ~4 nM
  
Polyinosinic-polycytidylic acid potassium
TLR3
       
TLR7 agonist 21 
TLR8, EC50: 5932 nM
   
human TLR7, EC50: 17.53 nM
mTLR7, EC50: 41.7 nM
  
TLR7 agonist 24     
TLR7, EC50: 3.72 μM
  
TLR7 agonist 9     
TLR7
  
TLR8 agonist 7 
TLR8
      
NF-κB-IN-14    
TLR4
   
ORN 02 
TLR8
      
FSL-1   
TLR2
   
TLR6
Vidutolimod  
TLR9
     
TLR7 agonist 27     
TLR7, EC50: 238.1 nM
  
Macrophage-activating lipopeptide 2   
TLR2
   
TLR6
TLR8 agonist 8 
TLR8
      
Tri(TLR4-IN-C34-C2-amide-PEG1)-amide-C3-COOH    
TLR4
   
Pam3CSK4-Biotin   
TLR2
  
TLR1
 
TLR7 agonist 5     
TLR7, EC50: ~4 nM
  
ODN M326  
TLR9
     
TLR8 agonist 9 
TLR8
      
TLR7/8 agonist 11 
TLR8, EC50: 13.1 nM
   
human TLR7, EC50: 31.1 nM
  
TLR2 agonist 1   
hTLR2, EC50: 116 pM
    
Xanthine oxidase-IN-6    
TLR4
   
ORN 02 sodium 
TLR8
      
3M-011 
TLR8
   
TLR7
  
MTT5     
TLR7
  
M199
TLR3
 
TLR9
     98.55%
Rabeximod   
TLR2
TLR4
   
P53/TLR2 modulator-1   
TLR2
    
TLR7 agonist 8     
TLR7, EC50: ~4 nM
  
TLR7/8 agonist 9 
TLR8
   
TLR7
  
TLR7 agonist 26     
TLR7, EC50: 225.5 nM
  
Cholesterol oxidase, rhodococcus sp   
TLR2
    
TLR7 agonist 14     
TLR7, IC50: 18 nM
  
UM-3006 
TLR8
   
TLR7
  
Isatoribine     
TLR7
  
AYK004-B1     
TLR7, EC50: 0.2265 nM
  
BBIQ (GMP)     
human TLR7, EC50: 59.1 nM
  
AYK004 
TLR8
   
TLR7
  
Creatine ethyl ester
TLR3
  
TLR2
TLR4
TLR7