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TLR

Toll-like receptors (TLRs) are a class of proteins that play a key role in the innate immune system. They are single-pass membrane-spanning receptors usually expressed on sentinel cells such as macrophages and dendritic cells, that recognize structurally conserved molecules derived from microbes.

  • Chloroquine
    T868954-05-7
    Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.
    • $54
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  • Polyinosinic-polycytidylic acid
    T2317124939-03-5
    Polyinosinic-polycytidylic acid (Poly(I:C)) is a double-stranded RNA (dsRNA) and a TLR3 agonist. Polyinosinic-polycytidylic acid induces natural immunity in mammals.
    • $45
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  • Pam3CSK4 TFA (112208-00-1 free base)
    TP1067112208-01-2
    Pam3CSK4 TFA (Pam3Cys-Ser-(Lys)4 TFA) is an agonist of toll-like receptor 1/2 (TLR1/2) (EC50 of 0.47 ng/mL for human TLR1/2).
    • $128
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  • TLR7/8-IN-1
    T380782205095-75-4
    TLR7/8-IN-1, a crystalline TLR7/TLR8 inhibitor, is a valuable compound for autoimmune disease research[1].
    • $189
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  • Chloroquine phosphate
    T019450-63-5
    Chloroquine phosphate (Aralen phosphate) is an aminoquinoline antimalarial and also is widely used as an autophagy inhibitor. Chloroquine also is an inhibitor of toll-like receptors (TLRs).
    • $42
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  • Chloranil
    T80673118-75-2
    Chloranil (tetrachloro-p-benzoquinone) triggers inflammation and neurological dysfunction through Toll-like receptor 4 signaling and can be used to model inflammation in mice.
    • $30
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  • Hydroxychloroquine
    T9287118-42-3
    Hydroxychloroquine (2-[[4-[(7-Chloroquinolin-4-yl)amino]pentyl](ethyl)amino]ethanol) (HCQ) is an alkalinizing lysosomatropic drug that acts by inducing apoptosis of renal cancer cells in vitro and inhibiting TLR7/9. It is a medication used to prevent and treat malaria, and it's also being studied as an experimental treatment for COVID-19.
    • $30
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  • DSR-6434
    T111081059070-10-8In house
    DSR-6434 is a selective agonist of TLR7 with antitumor effect. DSR-6434 exhibits EC50s of 7.2 nM and 4.6 nM for human and mouse.
    • $58
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  • RS09 2TFA (1449566-36-2 free base)
    TP1938L
    RS09 2TFA (1449566-36-2 free base) is a TLR4 agonist. Promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. It acts as an adjuvant in vivo and enhances X-15 specific antibody serum concentrations.
    • $137
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  • Rabeximod
    T34249872178-65-9In house
    Rabeximod is a potent immunomodulator that reduces the severity of autoimmune diseases in rat models. Rabeximod inhibits arthritis in a time-dependent manner by stimulating TLR2 and TLR4 downstream to block the activation of inflammatory cells, most likely macrophages. Rabeximod effectively reduces brain antigen presentation in mice during anti-inflammatory therapy for traumatic brain injury.
    • $258
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  • VB 201
    T29099L630112-41-3In house
    VB 201 is an oxidized phospholipid small molecule with anti-inflammatory activity that inhibits CD14 and Toll-like receptor 2-dependent innate cell activation and limits atherosclerosis, and can be used to study atherosclerosis.
    • $195
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  • Isatoribine
    T24178122970-40-5In house
    Isatoribine(ANA245) free base is a potent TLR7 receptor agonist with anti-hepatitis C virus infection activity for the study of HCV infection.
    • $258
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  • TLR7/8/9 antagonist 2
    T720352920729-91-3In house
    TLR7/8/9 antagonist 2 is an orally active and highly bioavailable vTLR7/8/9 antagonist. TLR7/8/9 antagonist 2 inhibits HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC50s of 0.011 μM, 0.029 μM and 0,052 μM, respectively. TLR7/8/9 antagonist 2 can be used to study auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis.
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    • ABR-238901
      T391151638200-22-2In house
      ABR-238901 is an oral, active S100A8/A9 blocker that inhibits the interaction of S100A8/A9 with its receptors RAGE(receptor for advanced glycation end products) and TLR4 (toll-like receptor 4). ABR-238901 has potential as a compound for the treatment of myocardial infarction (MI).
      • $125
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    • AZD8848
      T10437866269-28-5In house
      AZD8848 is a selective antedrug agonist of toll-like receptor 7 (TLR7). It is developed for the research of asthma and allergic rhinitis.
      • $1,620
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    • Selgantolimod
      T168702004677-13-6In house
      Selgantolimod is an effective and selective toll-like receptor 8 agonists for the treatment of the hepatitis B virus and human immunodeficiency virus infection.
      • $1,820
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    • CU-115
      T96452471982-20-2In house
      CU-115 is a selective and potent TLR8 antagonist with IC50 of 1.04 µM and =>50 µM for TLR8 and TLR7, respectively. CU-115 decreases production of TNF-α and IL-1β activated by R-848 in THP-1 cells.
      • $53
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    • Enpatoran
      T95702101938-42-3In house
      Enpatoran is an inhibitor of TLR7(IC50 = 11.1 nM) and TLR8(IC50 = 24.1 nM). Enpatoran was found to be inactive against TLR3, TLR4, and TLR9 in vitro and in vivo.
      • $122
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    • CU-CPD107
      T353492573912-32-8In house
      CU-CPD107 is a selective agonist of toll-like receptor 8 (TLR8) and also shows activation activity against ssRNA ligands. CU-CPD107 acts as an inhibitor of TLR8 signaling in the presence of R848 (IC50=13.7 μM). CU-CPD107 exhibited coagonist activity in the presence of ssRNA, while CU-CPD107 alone could not affect TLR8 signal transduction.
      • $64
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    • CL264
      T108331510712-69-2In house
      CL264, a selective agonist of TLR7, can be used in studies about innate immune signals.
      • $79
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    • Imiquimod
      T013499011-02-6
      Imiquimod (R 837) is an immune response modifier that acts as a toll-like receptor 7 agonist.
      • $37
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    • Resiquimod
      T6964144875-48-9
      Resiquimod (R848) is an imidazoquinoline amine and Toll-like receptor (TLR) agonist with potential immune response modifying activity. Resiquimod exerts its effect through the TLR signaling pathway by binding to and activating TLR7 and 8 mainly on dendritic cells, macrophages, and B-lymphocytes. This induces the nuclear translocation of the transcription activator NF-kB as well as activation of other transcription factors. This may lead to an increase in mRNA levels and subsequent production of cytokines, especially interferon-alpha (INF-a) and other cytokines, thereby enhancing T-helper 1 (Th1) immune responses. In addition, topical application of resiquimod appears to activate Langerhans' cells, leading to an enhanced activation of T-lymphocytes.
      • $30
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    • Hydroxychloroquine sulfate
      T0951747-36-4
      Hydroxychloroquine sulfate (Acidum iopanoicum) inhibits plasmodial heme polymerase. It is a chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa.
      • $48
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    • C29
      T3502363600-92-4
      C29 is a novel inhibitor of TLR2/1 and TLR2/6 signaling induced by synthetic and bacterial TLR2 agonists in human HEK-TLR2 and THP-1 cells, but only TLR2/1 signaling in murine macrophages.
      • $47
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    • Resatorvid
      TQ0181243984-11-4
      Resatorvid (TAK-242) is a selective inhibitor of Toll-like receptor 4 (TLR4). Resatorvid binds directly to Cys747 and prevents TLR4 from binding to TIRAP, thereby blocking downstream signaling. Resatorvid has antitumor activity, anti-inflammatory activity, and neuroprotective effects.
      • $45
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    • MyD88-IN-1
      T773532911609-80-6
      MyD88-IN-1 is a potent MyD88 inhibitor MyD88-IN-1 has anti-inflammatory activity and inhibits downstream inflammatory signaling pathways, including the NF-κB pathway, of members of the Toll-like receptor (TLR) and interleukin-1 (IL-1) receptor family MyD88-IN-1 may be used for the study of cancer and the treatment of inflammation.
      • $48
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    • CpG ODN 10101
      T748741234402-77-7
      CpG ODN 10101 (CPG 10101) is a novel potent and selective Toll-like receptor 9 (TLR9)-containing oligodeoxynucleotide agonist with antiviral activity for the treatment of chronic infections.
      • $310
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    • SM-276001
      T12933473930-22-2
      SM-276001 is a potent selective agonist of TLR7,and is an orally active interferon (IFN) inducer.
      • $135
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    • Semapimod tetrahydrochloride
      T35593164301-51-3
      Semapimod tetrahydrochloride (CPSI-2364 tetrahydrochloride) is a synthetic ornithine mitogen-activated protein kinase blocker and pro-inflammatory cytokine production inhibitor that interferes with macrophage and microglia function. Sematimod tetrahydrochloride inhibits TLR4 signaling, TNF-α, IL-1β, and IL-6, and is used in the study of Crohn's disease and other inflammatory conditions.
      • $99
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    • Tomaralimab
      T769751449294-76-1
      Tomaralimab (OPN-305) is a humanized IgG4 monoclonal antibody targeting TLR2. Tomarlimab is used to study myelodysplastic syndromes (MDS).
      • $222
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    • Capillarisin
      TN358756365-38-9
      Capillarisin is a novel blocker of STAT3 activation and thus may have a potential in negative regulation of growth, metastasis, and chemoresistance of tumor cells, it inhibits cancer cell growth of osteosarcoma cells by inducing apoptosis accompanied with
      • $2,169
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    • Pam2CSK4 TFA
      TP2282L
      Pam2CSK4 TFA (PUL-042 TFA) is a potent dual agonist of TLR2 and TLR6, a peptide that mimics bacterial lipoproteins.Pam2CSK4 TFA promotes platelet aggregation, and can be used to study the effects of lipoproteins on the periodontium.
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      • RS 09
        TP19381449566-36-2
        TLR4 agonist. Promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. Acts as an adjuvant in vivo; enhances X-15 specific antibody serum concentrations, when administered with X-15-KLH in mice.
          5 days
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        • Polygalasaponin F
          T3826882664-74-6
          Polygalasaponin F has anti-neuroinflammatory activity, can inhibit the release of inflammatory cytokines TNF-α and NO induced by lipopolysaccharides (LPS) and reduce the expression of inducible nitric oxide synthases. Polygalasaponin F can significantly i
          • $100
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        • BMS-905
          T600522205846-49-5
          BMS-905 is a potent dual inhibitors of TLR7 and TLR8 with good selectivity against TLR9 and other family members. BMS-905 can be used in studies about the treatment of diseases such as psoriasis, arthritis, and lupus.
          • $68
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        • CU-CPT-9a
          T73172165340-32-7
          CU-CPT-9a is a potent TLR8 inhibitor (IC50 : 0.5 nM), that suppresses TLR8-mediated proinflammatory signaling in various cell lines and human primary cells-
          • $34
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        • E6446 dihydrochloride
          T40681345675-25-3
          E6446 dihydrochloride is a novel synthetic antagonist for nucleic acid-sensing TLRs; potently suppressed DNA stimulation of HEK:TLR9 cells with IC50 of 10 nM.
          • $109
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        • PF-4878691
          T16506532959-63-0
          PF-4878691 (3M-852A) is an effective and selective Toll-like receptor 7 agonists modelled. It is used to dissociate its antiviral and inflammatory activities.
          • $147
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        • Pepinh-TRIF TFA
          T76089
          Pepinh-TRIF TFA is a 30 aa peptide associated with the immune system that blocks TRIF signaling by interfering with TLR-TRIF interaction (TLR-TRIF interaction ).
          • $128
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        • Loxoribine
          T15777121288-39-9
          Loxoribine (RWJ 21757) is a guanosine analog. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist. It has anti-viral and anti-tumor activities.Loxoribine is a potent new immunostimulant with a relatively broad spectrum of immunobiological activities.
          • $43
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        • Bropirimine
          T552156741-95-8
          Bropirimine (U-54461) (U-54461) is a biological response modifier that is thought to act through the induction of lymphokines.
          • $68
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        • Afimetoran
          T396542171019-55-7
          Afimetoran (BMS-986256) is a toll-like receptor antagonist. Afimetoran can be used in the research of inflammatory and autoimmune diseases.
          • $84
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        • TLR7/8/9-IN-1
          T396692180127-82-4
          TLR7/8/9-IN-1 is a potent inhibitor of Toll-like receptors 7/8/9 (TLR7/8/9) with an IC50 of 43 nM.
          • $73
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        • Vesatolimod
          T68461228585-88-3
          Vesatolimod (GS-9620) is an effective and specific orally active agonist of Toll-like receptor 7.
          • $45
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        • Schaftoside
          T389851938-32-0
          Schaftoside (APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE) has antioxidant and anticancer activity.
          • $40
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        • TLR3-IN-1
          T226981279713-77-7
          TLR3-IN-1 (CU CPT 4a) is a selective TLR3 inhibitor (IC50: 3.44 μM in RAW 264.7 cells). It can inhibit TLR3/dsRNA complex-mediated downstream signaling pathways and inhibit the production of TNF-α and IL-1β in whole cells.
          • $48
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        • IAXO-102
          T115981115270-63-7
          IAXO-102 is a TLR4 antagonist that negatively regulates TLR4 signaling. It inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein. IAXO-102 also prevents experimental abdominal aortic aneurysm development.
          • $89
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        • Toll-like receptor modulator
          T13182926927-42-6
          Toll-like receptor modulator is a TLR7/8 modulator, which modulates immune function.
          • $65
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        • Atractylenolide I
          T5S016773069-13-3
          1. Atractylenolide-I has an anti-inflammatory effect by inhibiting TNF-α and IL-6 production; ameliorates sepsis syndrome, liver and kidney functions by reduction of pro-inflammatory cytokines and LPS. 2. Atractylenolide-I significantly sensitizes the res
          • $36
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        • Leonurine hydrochloride
          T408024735-18-0
          Leonurine hydrochloride (SCM-198 hydrochloride) , a major alkaloid compound extracted from Leonurus japonicas Houtt. (Labiatae), is considered to have antitumor roles.
          • $31
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