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-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
  • HY-B0180R
    Imiquimod (Standard)
    Agonist
    Imiquimod (Standard) is the analytical standard of Imiquimod. This product is intended for research and analytical applications. 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.
    Imiquimod (Standard)
  • HY-N1346R
    Robinin (Standard)
    Inhibitor
    Robinin (Standard) is the analytical standard of Robinin. This product is intended for research and analytical applications. 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.
    Robinin (Standard)
  • HY-B0180C
    Imiquimod dihydrochloride
    Agonist
    Imiquimod (R 837) dihydrochloride, 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.
    Imiquimod dihydrochloride
  • HY-D1056A4
    Lipopolysaccharides, from E. coli O128:B12
    Activator
    Lipopolysaccharides, from E. coli O128:B12 (LPS, from Escherichia coli (O128:B12)) are endotoxins and TLR4 activators extracted from Escherichia coli (E. coli O128:B12) and are classified as S (smooth) type LPS. Lipopolysaccharides, from E. coli O128:B12 possess the typical three-part structure: O-antigen, R3-type core oligosaccharide, and lipid A. Lipopolysaccharides, from E. coli O128:B12 activate TLR-4 in immune cells, can be used to construct animal models of neonatal brain inflammation, and may influence preterm birth in neonates.
    Lipopolysaccharides, from E. coli O128:B12
  • HY-P10718
    IMG-2005
    Inhibitor
    IMG-2005 is a TLR signaling pathway inhibitor. IMG-2005 mimics the Toll/interleukin-1 receptor (TIR) domain of MyD88, thereby preventing its homodimerization, which causes damage to tracheal epithelial cells and triggers pulmonary immune diseases.
    IMG-2005
  • HY-111582G
    BBIQ (GMP)
    Agonist
    BBIQ (GMP) is BBIQ (HY-111582) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. BBIQ is a potent and selectively toll-like receptor 7 (TLR7) agonist with an EC50 of  59.1 nM. BBIQ is a powerful vaccine adjuvant that enhances innate immune responses.
    BBIQ (GMP)
  • HY-159671A
    3D-Monophosphoryl Lipid (14) triethylamine
    Agonist
    3D-Monophosphoryl Lipid (14) (3D-Monophosphoryl Lipid (14)) triethylamine is a TLR agonist that can be used as a vaccine adjuvant to enhance the immunogenicity of vaccines.
    3D-Monophosphoryl Lipid (14) triethylamine
  • HY-D1056D
    Lipopolysaccharides, from P. gingivalis
    Lipopolysaccharides, from P. gingivalis (LPS, from Porphyromonas gingivalis) are endotoxins and TLR4 activators extracted from Porphyromonas gingivalis (P. gingivalis) and are classified as S (smooth) type LPS. Lipopolysaccharides, from P. gingivalis possess the typical three-part structure: O-antigen, core oligosaccharide, and lipid A. Lipopolysaccharides, from P. gingivalis activate TLR-4 in immune cells and are important virulence factors in the mechanism of periodontal disease. Lipopolysaccharides, from P. gingivalis can be used in research related to periodontitis.
    Lipopolysaccharides, from P. gingivalis
  • HY-159672B
    3D-Monophosphoryl Lipid (12,16) triethylamine
    Agonist
    3D-Monophosphoryl Lipid (12,16) (triethylamine) is a TLR agonist that can be used as a vaccine adjuvant to enhance the immunogenicity of vaccines.
    3D-Monophosphoryl Lipid (12,16) triethylamine
  • HY-162579
    TLR7 agonist 22
    Agonist
    TLR7 agonist 22 (Compound 11a) emerges as a selective TLR7 agonist with an IC50 value of 25.86 μM. TLR7 agonist 22 inhibits the cellular HBsAg secretion and effectively activates TLR7, thereby inducing the secretion of TLR7-regulated cytokines IL-12, TNF-αand IFN-αin human PBMC cells. TLR7 agonist 22 is a promising for research in the field of developing novel immunomodulatory anti-HBV agents.
    TLR7 agonist 22
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) Inducers, Inhibitors, Agonists, Antagonists, Activators & Modulators
Product NameTLR3TLR8TLR9TLR2TLR4TLR7TLR1TLR6Purity    
Lipopolysaccharides, from E. coli O55:B5    
TLR4
   
Resiquimod 
TLR8
   
TLR7
  99.95%
Resatorvid    
TLR4
   99.95%
Imiquimod     
TLR7
  99.96%
C29   
TLR2
    ≥98.0%
Pam3CSK4 TFA   
TLR2
  
TLR1
 99.66%
Hydroxychloroquine sulfate  
TLR9
  
TLR7
  99.99%
Agatolimod sodium  
TLR9
     98.49%
CU-CPT 4a
TLR3, IC50: 3.44 μM (in RAW 264.7 cells)
       99.34%
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
     
Diprovocim   
TLR2
  
TLR1
 98.82%
CU-CPT22   
TLR2
  
TLR1
 ≥99.0%
Imiquimod hydrochloride     
TLR7
  99.77%
TLR4-IN-C34    
TLR4
   99.90%
Agatolimod  
TLR9
     
Motolimod 
TLR8
      98.12%
Telratolimod 
TLR8
   
TLR7
  98.98%
Thiamine hydrochloride    
TLR4
   99.97%
Atractylenolide I  
TLR9
  
TLR7
  99.94%
Physcion    
TLR4
   99.10%
Vesatolimod     
TLR7
  99.90%
Schaftoside    
TLR4
   99.67%
MMG-11   
TLR2
    99.24%
AT791  
TLR9, IC50: 0.04 μM
  
TLR7, IC50: 3.33 μM
  98.77%
ODN 2216  
TLR9
     
Enpatoran hydrochloride 
TLR8, IC50: 24.1 nM
   
TLR7, IC50: 11.1 nM
  99.33%
CU-T12-9   
TLR2, EC50: 52.9 nM (in HEK-Blue cells)
  
TLR1, EC50: 52.9 nM (in HEK-Blue cells)
 99.96%
ODN 1018  
TLR9
     
Selgantolimod 
TLR8
      98.23%
ODN 2395 sodium  
TLR9
     98.20%
ODN 1668 sodium  
TLR9
     98.79%
ODN 2395  
TLR9
     98.39%
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
     99.80%
Okanin    
TLR4
   99.98%
FSL-1 TFA   
TLR2
   
TLR6
99.65%
RS 09    
TLR4
   99.88%
Gardiquimod 
TLR8
   
TLR7
  99.91%
TLR7/8-IN-1 
TLR8
   
TLR7
  99.92%
D-Glucuronic acid    
TLR4
   
RS 09 TFA    
TLR4
   99.81%
CL075 
TLR8
      99.25%
ODN 1668  
TLR9
     98.79%
IAXO-102    
TLR4
   ≥98.0%
ssRNA40 sodium 
TLR8
   
TLR7
  
MD2-IN-1    
TLR4
   99.89%
Teneligliptin hydrobromide hydrate    
TLR4
   99.87%
Isofraxidin    
TLR4
   99.00%
TLR7/8 agonist 1 
TLR8
   
TLR7
  
E6446 dihydrochloride  
TLR9
  
TLR7
  99.96%
Robinin   
TLR2
TLR4
   98.77%
Loxoribine     
TLR7
  99.64%
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%
CU-CPT-9a 
TLR8, IC50: 0.5 nM
      99.36%
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)
  99.55%
AN-3485
TLR3
  
TLR2
TLR4
   
CU-CPT-8m 
TLR8, IC50: 67 nM
      99.98%
L48H37    
TLR4
   
L6H21    
TLR4
   99.46%
Procyanidin B3    
TLR4
   99.92%
CpG ODN 10101  
TLR9
     
CU-CPT17e
TLR3
TLR8
TLR9
     99.00%
CL264     
TLR7
  98.63%
Kaempferol 3-O-sophoroside   
TLR2
TLR4
   99.84%
Chloranil    
TLR4
   98%
E6446  
TLR9
  
TLR7
  ≥98.0%
TLR7 agonist 3     
TLR7
  99.90%
ODN M362  
TLR9
     
ODN 20844  
TLR9
  
TLR7
  
Imiquimod maleate     
TLR7
  99.25%
CU-115 
TLR8, IC50: 1.04 μM
   
TLR7, IC50: 50 μM
  99.55%
RKH acetate    
TLR4
   99.45%
Magnesium citrate    
TLR4
   ≥98.0%
GSK2245035     
TLR7
  99.85%
Fosfenopril    
TLR4
   99.89%
CU-CPT9b 
TLR8, IC50: 0.7 nM
TLR8, Kd: 21 nM
      99.03%
Resiquimod (GMP) 
TLR8
   
TLR7
  
Hydroxychloroquine (sulfate) (Standard)  
TLR9
  
TLR7
  99.28%
Polygalasaponin F    
TLR4
   99.85%
MAPK-IN-1    
TLR4
   
PF-4878691     
TLR7
  99.89%
TLR7/8 agonist 4 
TLR8
   
TLR7
  99.04%
AZD8848     
TLR7
  99.14%
SM-324405     
human TLR7, pEC50: 7.3
Rat TLR7, pEC50: 6.6
TLR7, EC50: 50 nM
  98.52%
1V209     
TLR7
  99.67%
LHC-165     
TLR7
  ≥98.0%
CL097 hydrochloride 
TLR8
   
TLR7
  99.90%
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%
E104     
TLR7
  
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
   
TLR7
  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%
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
  
TLR4/NF-κB-IN-1    
TLR4
   
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
     
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