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-17589A
    Chloroquine
    Inhibitor 99.50%
    Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
    Chloroquine
  • HY-D1056
    Lipopolysaccharides, from E. coli O55:B5
    Activator
    Lipopolysaccharides, from E. coli O55:B5 is an endotoxin extracted from E. coli O55:B5, consisting of an antigen-specific chain, A core oligosaccharide, and lipid A. Lipopolysaccharides, from E. coli O55:B5 activates TLR-4 of immune cells. Lipopolysaccharides, from E. coli O55:B5 can induce the change of body temperature in rats with dose and serotype specificity. Lipopolysaccharides, from E. coli O55:B5 caused a heterogeneous and dose-independent increase in body temperature in rats.
    Lipopolysaccharides, from E. coli O55:B5
  • HY-13740
    Resiquimod
    Agonist 99.95%
    Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α.
    Resiquimod
  • 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.
    Resatorvid
  • HY-107202
    Polyinosinic-polycytidylic acid
    Agonist 99.40%
    Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid can directly trigger cancer cells to undergo apoptosis.
    Polyinosinic-polycytidylic acid
  • HY-D1056A1
    Lipopolysaccharides, from E. coli O111:B4
    Lipopolysaccharides are lipopolysaccharide endotoxins and TLR-4 activators that activate pathogenicity-associated molecular patterns (PAMPs) of the immune system and induce cell secretion of migrasomes. Lipopolysaccharides can be extracted from the outer leaflet of the outer membrane of Gram-negative bacteria and are composed of an antigenic O-specific chain, a core oligosaccharide, and lipid A. Lipopolysaccharides, from E. coli O111:B4 is a kind of endotoxins derived from E. coli.
    Lipopolysaccharides, from E. coli O111:B4
  • HY-150745A
    ODN 24987 sodium
    ODN 24987 sodium is a Guanine-modified inhibitory oligonucleotides (ODN), targeting TLR9. ODN 24987 can inhibit IL-6 and IFN-α release. ODN 24987 sodium can be used for research immune disorders. ODN 24987 sequence: 5’-C-C-T-G-G-C-c7G-G-G-G-3’.
    ODN 24987 sodium
  • HY-P10586A
    Macrophage-activating lipopeptide 2 TFA
    Activator 98.60%
    Macrophage-activating lipopeptide 2 TFA is an agonist of Toll like receptors TLR-2/TLR-6. Macrophage-activating lipopeptide-2 enhances endothelial nitric oxide synthase (eNOS) phosphorylation and endothelial cell release of NO, thereby improving vasodilation. Macrophage-activating lipopeptide-2 enhances endothelial adhesion of white blood cells and improve perfusion recovery and collateral growth in the hind limbs of hypercholesterolemic Apoe deficient mice undergoing experimental femoral artery ligation (FAL).
    Macrophage-activating lipopeptide 2 TFA
  • HY-17589
    Chloroquine phosphate
    Inhibitor 99.89%
    Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
    Chloroquine phosphate
  • HY-W031727
    Hydroxychloroquine
    Inhibitor 99.77%
    Hydroxychloroquine (HCQ) is a synthetic oral antimalarial drug that can be used in the study of malaria and autoimmune diseases such as systemic lupus erythematosus and rheumatoid arthritis. Hydroxychloroquine is a potent autophagic flux inhibitor with antiviral activity (such as SARS-CoV-2 virus) that inhibits Toll-like receptor 7/9 (TLR7/9) signaling.
    Hydroxychloroquine
  • HY-100461
    C29
    Inhibitor ≥98.0%
    C29 is a Toll-like receptor 2 (TLR2) inhibitor. C29 blocks hTLR2/1 and hTLR2/6 signaling with IC50s of 19.7 and 37.6 μM, respectively.
    C29
  • HY-B0180
    Imiquimod
    Agonist 99.96%
    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
  • HY-153808
    Complete Freund's adjuvant (CFA)
    Complete Freund's adjuvant (CFA) is an immunoadjuvant emulsified with antigen by its discoverer Jules T. Freund to enhance an animal's immune response to an antigen. Complete Freund's adjuvant (CFA) is also an inducer of the Th1 immune response and a ligand of TLRs. Complete Freund's adjuvant (CFA) contains heat-killed inactive tuberculosis bacilli and consists of a paraffin oil-in-water emulsion. Complete Freund's adjuvant (CFA) stimulates a strong and durable immune response and can be used to induce persistent inflammatory pain models in mice, experimental autoimmune myocarditis (EAM) models, and more. Incomplete Freund's adjuvant (IFA) (HY-153808A) is another type of Freund's Adjuvant that stimulates a weaker immune response.
    Complete Freund's adjuvant (CFA)
  • HY-B1370
    Hydroxychloroquine sulfate
    Inhibitor 99.99%
    Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro.
    Hydroxychloroquine sulfate
  • HY-P1180A
    Pam3CSK4 TFA
    Agonist 99.66%
    Pam3CSK4 TFA is a toll-like receptor 1/2 (TLR1/2) agonist with an EC50 of 0.47 ng/mL for human TLR1/2.
    Pam3CSK4 TFA
  • HY-108473
    CU-CPT 4a
    Inhibitor 99.34%
    CU-CPT 4a (TLR3-IN-1) is a potent, highly selective TLR3 signaling inhibitor. CU-CPT 4a represses the expression of downstream signaling pathways mediated by the TLR3/dsRNA complex, including TNF-α and IL-1β.
    CU-CPT 4a
  • HY-134581
    Enpatoran
    Inhibitor 99.80%
    Enpatoran (M5049) 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 is inactive against TLR3, TLR4 and TLR9. Enpatoran can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran exhibits excellent pharmacokinetic properties in vivo. Enpatoran can be used for both innate and adaptive autoimmunity blocking research .
    Enpatoran
  • HY-150218
    Agatolimod sodium
    Agonist 98.49%
    Agatolimod sodium (ODN 2006) is a class B CpG ODN and is a TLR9 agonist. Agatolimod sodium can be used as vaccine adjuvant. Agatolimod sodium can be used for the research of cancer. Sequence: 5’-TCGTCGTTTTGTCGTTTTGTCGTT-3’.
    Agatolimod sodium
  • HY-146245
    ODN 1826
    Agonist
    ODN 1826 (CpG 1826), a class B CpG ODN (oligodeoxynucleotide), is a TLR9 agonist. ODN 1826 promotes Apoptosis. ODN 1826 is an excellent immune stimulator with antitumor activity. ODN 1826 has protective effects on the heart. ODN 1826 sequence: 5’-tccatgacgttcctgacgtt-3’.
    ODN 1826
  • HY-129522
    Sulfo-ara-F-NMN
    Activator 99.36%
    Sulfo-ara-F-NMN (CZ-48) is a mimetic of nicotinamide mononucleotide (NMN). Sulfo-ara-F-NMN acts selectively, activating SARM1 but inhibiting CD38 (IC50 around 10 μM). Sulfo-ara-F-NMN induces intracellular cyclic ADP-ribose (cADPR) production.
    Sulfo-ara-F-NMN
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
Product NameTLR3TLR8TLR9TLR2TLR4TLR7TLR1TLR6Purity    
Lipopolysaccharides, from E. coli O55:B5    
TLR4
   
Resiquimod 
TLR8
   
TLR7
  99.95%
Resatorvid    
TLR4
   99.95%
C29   
TLR2
    ≥98.0%
Imiquimod     
TLR7
  99.96%
Hydroxychloroquine sulfate  
TLR9
  
TLR7
  99.99%
Pam3CSK4 TFA   
TLR2
  
TLR1
 99.66%
CU-CPT 4a
TLR3, IC50: 3.44 μM (in RAW 264.7 cells)
       99.34%
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%
Agatolimod sodium  
TLR9
     98.49%
ODN 1826  
TLR9
     
ODN 1826 sodium  
TLR9
     99.51%
Diprovocim   
TLR2
  
TLR1
 98.82%
Imiquimod hydrochloride     
TLR7
  99.77%
Agatolimod  
TLR9
     
CU-CPT22   
TLR2
  
TLR1
 ≥99.0%
Polyinosinic-polycytidylic acid sodium
TLR3
       99.40%
TLR4-IN-C34    
TLR4
   99.90%
Telratolimod 
TLR8
   
TLR7
  98.98%
Motolimod 
TLR8
      98.12%
Atractylenolide I  
TLR9
  
TLR7
  99.94%
Physcion    
TLR4
   99.10%
ODN 2216  
TLR9
     
AT791  
TLR9, IC50: 0.04 μM
  
TLR7, IC50: 3.33 μM
  98.77%
Schaftoside    
TLR4
   99.67%
ODN 1018  
TLR9
     
CU-T12-9   
TLR2, EC50: 52.9 nM (in HEK-Blue cells)
  
TLR1, EC50: 52.9 nM (in HEK-Blue cells)
 98.94%
MMG-11   
TLR2
    99.11%
Enpatoran hydrochloride 
TLR8, IC50: 24.1 nM
   
TLR7, IC50: 11.1 nM
  99.33%
Selgantolimod 
TLR8
      98.23%
ODN 2395  
TLR9
     98.39%
Neoseptin 3    
TLR4, EC50: 18.5 μM
   99.57%
CL097 
TLR8
   
TLR7
  99.89%
ODN 2395 sodium  
TLR9
     
FSL-1 TFA   
TLR2
   
TLR6
99.65%
CL075 
TLR8
      99.25%
Sparstolonin B   
TLR2
TLR4
   99.54%
Okanin    
TLR4
   99.98%
ODN 1668  
TLR9
     
D-Glucuronic acid    
TLR4
   
TLR9-IN-1  
human TLR9, IC50: 7 nM
     99.80%
TLR7/8-IN-1 
TLR8
   
TLR7
  99.92%
ODN 1668 sodium  
TLR9
     ≥99.0%
Robinin   
TLR2
TLR4
   98.77%
Gardiquimod 
TLR8
   
TLR7
  99.91%
Teneligliptin hydrobromide hydrate    
TLR4
   99.87%
IAXO-102    
TLR4
   ≥98.0%
MD2-IN-1    
TLR4
   99.89%
Isofraxidin    
TLR4
   99.00%
Loxoribine     
TLR7
  99.64%
Gardiquimod diTFA 
TLR8
   
TLR7
  ≥99.0%
E6446 dihydrochloride  
TLR9
  
TLR7
  99.96%
TLR7/8 agonist 1 
TLR8
   
TLR7
  
Monophosphoryl lipid A    
TLR4
   ≥99.0%
NecroX-7    
TLR4
   99.69%
L48H37    
TLR4
   
CpG ODN 10101  
TLR9
     
CL264     
TLR7
  98.63%
CU-CPT-9a 
TLR8, IC50: 0.5 nM
      99.36%
CU-CPT-8m 
TLR8, IC50: 67 nM
      99.98%
CAY10614    
TLR4, IC50: 1.675 μM (in HEK293 cells)
   98.04%
TLR7/8 agonist 3 
TLR8
   
TLR7
  99.96%
DSR-6434     
TLR7, EC50: 7.2 nM (Human)
TLR7, EC50: 4.6 nM (Mice)
  99.55%
Procyanidin B3    
TLR4
   99.92%
CU-CPT17e
TLR3
TLR8
TLR9
     99.00%
Kaempferol 3-O-sophoroside   
TLR2
TLR4
   99.84%
TLR7 agonist 3     
TLR7
  99.90%
AN-3485
TLR3
  
TLR2
TLR4
   
ssRNA40 sodium 
TLR8
   
TLR7
  
L6H21    
TLR4
   99.46%
GSK2245035     
TLR7
  99.85%
ODN M362  
TLR9
     
ODN 20844  
TLR9
  
TLR7
  
CU-115 
TLR8, IC50: 1.04 μM
   
TLR7, IC50: 50 μM
  99.55%
Imiquimod maleate     
TLR7
  99.25%
LHC-165     
TLR7
  ≥98.0%
Fosfenopril    
TLR4
   99.89%
CU-CPT9b 
TLR8, IC50: 0.7 nM
TLR8, Kd: 21 nM
      99.03%
RKH acetate    
TLR4
   99.45%
E6446  
TLR9
  
TLR7
  ≥98.0%
TLR7/8 agonist 4 
TLR8
   
TLR7
  99.04%
Resiquimod (GMP) 
TLR8
   
TLR7
  
Polygalasaponin F    
TLR4
   99.85%
PF-4878691     
TLR7
  99.89%
Chloranil    
TLR4
   98%
1V209     
TLR7
  99.67%
AZD8848     
TLR7
  99.14%
TLR7 agonist 6     
TLR7, EC50: ~4 nM
  98.08%
MAPK-IN-1    
TLR4
   
SM-324405     
human TLR7, pEC50: 7.3
Rat TLR7, pEC50: 6.6
TLR7, EC50: 50 nM
  98.52%
Resiquimod-d5 
TLR8
   
TLR7
  99.84%
TLR7 agonist 1     
TLR7, IC50: 90 nM
  98.95%
MMG-11 quarterhydrate   
TLR2
    99.09%
CL097 hydrochloride 
TLR8
   
TLR7
  99.90%
ODN 24987  
TLR9
     
BBIQ     
TLR7, EC50: 59.1 nM (Human TLR7)
  99.85%
SMU-L11     
TLR7, EC50: 0.024 μM
  99.64%
FAM-labeled ODN 1826 sodium  
TLR9
     98.03%
E104     
TLR7
  
TLR4-IN-C34-C2-amide-C6-OH    
TLR4
   99.62%
Kdo2-Lipid A ammonium    
TLR4
   99.00%
ORN 06 sodium     
TLR7
  
Hydroxychloroquine (sulfate) (Standard)  
TLR9
  
TLR7
  99.28%
Diprovocim-X   
TLR2
  
TLR1
 98.64%
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%
Pam3CSK4   
TLR2
  
TLR1
 
TLR7 agonist 20 hydrochloride 
TLR8, EC50: 17.21 μM
   
TLR7, EC50: 0.23 μM
  99.86%
ODN 24888  
TLR9
  
TLR7
  
PVP-037.2 
TLR8
   
TLR7
  
TLR7/8 agonist 8 
TLR8, EC50: 12 nM
   
TLR7, EC50: 27 nM
  98.69%
(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
   
Mumefural    
TLR4
   
TLR7 agonist 17     
human TLR7, EC50: 12 nM
mTLR7, EC50: 17 nM
  
ORN 06     
TLR7
  
Eritoran    
TLR4
   
WYJ-2   
TLR2
    
TLR7 agonist 20 
TLR8, EC50: 17.21 μM
   
TLR7, EC50: 0.23 μM
  
TLR7-IN-1     
TLR7, IC50: 0.001 μM
  
Tri(TLR4-IN-C34-C2-amide-C3-amide-PEG1)-amide-C3-COOH    
TLR4
   
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
   
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