TLR

TLR製品

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  • TLR阻害剤 (17)
  • TLR抗体(3)
  • TLR活性剤(2)
  • TLR拮抗剤(4)
  • TLR作動薬(8)
  • 新製品
製品コード 製品名称 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S4157 Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).
Nat Commun, 2024, 15(1):1642
Cancer Lett, 2024, 604:217258
Phytomedicine, 2024, 135:156053
S6999 Chloroquine Chloroquine is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.
Signal Transduct Target Ther, 2024, 9(1):65
Mol Cancer, 2024, 23(1):240
Bioact Mater, 2024, 32:277-291
S4430 Hydroxychloroquine (HCQ) Sulfate Hydroxychloroquine (HCQ) Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
Redox Biol, 2024, 75:103274
Phytomedicine, 2024, 10.1016/j.phymed.2023.155152
Breast Cancer Res, 2024, 26(1):33
S7455 Resatorvid (TAK-242) Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 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.
Cancer Cell, 2024, S1535-6108(24)00119-3
Nat Commun, 2024, 15(1):7662
Redox Biol, 2024, 70:103072
S8133 Resiquimod (R-848) Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. Resiquimod reduces hepatitis C virus (HCV) infection. Phase 2.
Int J Nanomedicine, 2024, 19:3589-3605
Front Immunol, 2024, 15:1331480
Biology (Basel), 2023, 12(2)318
S7161 Motolimod Motolimod is a selective and potent Toll-like receptor 8 (TLR8) agonist with EC50 of 100 nM, > 50-fold selectivity over TLR7. Phase 2.
J Pharmacol Exp Ther, 2024, 388(3):751-764
Cell Rep, 2021, 35(7):109143
J Leukoc Biol, 2020, 1
S8677 Cu-CPT22 CU-CPT22 shows dose-dependent inhibitory effects blocking Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 ± 0.09 µM while no significant inhibition to TLR2/6. It demonstrates minimal non-specific inhibition against a panel of 10 representative kinases (PDGFRB, MET, DDR2, SRC, MAPK1, PAK1, AKT1, PKC-γ, CAMK1, and PLK4).
Cancer Cell, 2024, S1535-6108(24)00135-1
J Exp Clin Cancer Res, 2023, 42(1):172
J Exp Clin Cancer Res, 2023, 42(1):172
S7221 Vesatolimod (GS-9620) Vesatolimod (GS-9620) is a potent and selective orally active small molecule agonist of Toll-like receptor 7.
PLoS Pathog, 2022, 18(3):e1010354
J Pharm Biomed Anal, 2020, 179:112987
Stem Cell Res Ther, 2019, 10(1):387
S6597 TLR2-IN-C29 TLR2-IN-C29 (C29) is a Toll-like receptor 2 (TLR2) inhibitor that inhibits TLR2/1 and TLR2/6 signaling.
J Immunother Cancer, 2024, 12(6)e009082
Clin Immunol, 2024, 263:110226
PLoS Pathog, 2024, 20(11):e1012614
S6573 MD2-IN-1 MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD value of 189 μM.
Life Sci Alliance, 2023, 6(3)e202201636
Front Immunol, 2022, 13:995791
Br J Pharmacol, 2021, 10.1111/bph.15412
S7850 Lipopolysaccharides Lipopolysaccharides (LPSs, Endotoxin,LPS) is an endotoxin derived from the outer leaflet of the outer membrane of Gram-negative bacteria. Lipopolysaccharides consists of an antigen O-specific chain, a core oligosaccharide and lipid A. Lipopolysaccharides is a pathogenic associated molecular pattern (PAMP) that activates the immune system. Lipopolysaccharides activates TLR-4 on immune cells. Lipopolysaccharides induces secretion of cell migrasome.
Int Immunopharmacol, 2024, 137:112426
Biomolecules, 2024, 14(7)741
Sci Rep, 2024, 14(1):13102
S3924 Ginsenoside Rb1 Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS.
J Biol Chem, 2024, 300(8):107542
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
J Biol Chem, 2021, S0021-9258(21)00790-0
S8562 IRAK4-IN-2 IRAK4-IN-2 is a reversible kinase inhibitor that modulates IRAK4 function in both the toll-like receptor (TLR) and interleukin 1 receptor (IL-1R) signaling cascades.
Cancer Lett, 2021, 503:75-90
Cancer Lett, 2021, 503:75-90
S2979 CU-T12-9 CU-T12-9 is a specific agonist of Toll-like receptor (TLR) 1/2 with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.
Biomedicine & Pharmacotherapy, 2023, 114638
Biomed Pharmacother, 2023, 162:114638
S0716 E6446 E6446 is an inhibitor of Toll-like receptor (TLR) 7 and 9 signaling in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro.
Cancer Cell, 2024, S1535-6108(24)00135-1
Front Immunol, 2024, 15:1354055
JCI Insight, 2023, 8(22)e171054
S0822 TLR4-IN-C34 TLR4-IN-C34 (TLR4-C34, C34, TLR4-C34-IN) is a potent and selective antagonist of Toll-like receptor 4 (TLR4). TLR4-IN-C34 reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.
Exp Mol Med, 2024, 56(2):408-421.
J Immunother Cancer, 2024, 12(6)e009082
Am J Physiol Gastrointest Liver Physiol, 2024, 327(6):G741-G753
S0494 SM 324405 SM 324405 (compound 9e) is a potent and selective Toll-like receptor 7 (TLR7) agonist with EC50 of 50 nM.
S0002 IAXO-102 IAXO-102 is an antagonist of TLR4 targeting both MD-2 and CD14 co-receptors. IAXO-102 inhibits MAPK and p65 NF-κB phosphorylation and downregulates the expression of TLR4 dependent proinflammatory proteins. IAXO-102 inhibits experimental abdominal aortic aneurysm (AAA) development.
S9937 CU-CPD107 CU-CPD107 is a selective, dual-activity small-molecule which demonstrated differential activity against the TLR8 agonists and ssRNA ligands. In the presence of R848, CU-CPD107 acts as a TLR8 signaling inhibitor (IC50=13.7 μM). In the presence of ssRNA, CU-CPD107 shows synergistic agonist activities, while CU-CPD107 alone is unable to influence TLR8 signaling.
S9234 Schaftoside Schaftoside, a bioactive compound found in the Herba Desmodii Styracifolii, exhibits pancreatic lipase inhibitory activity. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission.
S0078 1V209 (TLR7 agonist T7) 1V209 (T7, TLR7 agonist T7) is an agonist of Toll-like receptor 7 (TLR7) with anti-tumor effects. 1V209 can be used as vaccine adjuvants, enhances antigen specific humoral and cellular immune responses.
S9623 Telratolimod Telratolimod (3M-052, MEDI9197) is an agonist of toll-like receptor 7 (TLR-7) and toll-like receptor 8 (TLR-8) with antitumor activity.
S6934 AMG-9810 AMG-9810 is a potent, competitive and selective vanilloid receptor 1 (TRPV1) antagonist and inhibits capsaicin activation with IC50 of 24.5 nM and 85.6 nM for human TRPV1 and rat TRPV1, repectively. AMG-9810 blocks all known modes of TRPV1 activation, including protons-, heat-, and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG-9810 significantly reduces the mRNA expression of TLR2 and TLR4. AMG-9810 also promotes mouse skin tumorigenesis mediated through EGFR/Akt/mTOR signaling.
S9931 Enpatoran Hydrochloride Enpatoran (M5049) hydrochloride is a potent, orally active, and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM, respectively, in HEK293 cells.
S0139 MD2-TLR4-IN-1 MD2-TLR4-IN-1 (Compound 22m) is a potent inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4). MD2-TLR4-IN-1 (compound 22m) inhibits lipopolysaccharide (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 of 0.89 μM and 0.53 μM, respectively.
E0639 TLR7/8 agonist 1 dihydrochloride TLR7/8 agonist 1 dihydrochloride is a toll-like receptor TLR7/TLR8 dual-agonistic imidazoquinoline.TLR7/8 agonist 1 retains TLR7-agonistic activity with an EC50 of 20 nM.
A2696 Anti-TLR3 / CD283 (CNTO5429) Anti-TLR3 / CD283 (CNTO5429) is a novel antibody that binds to the extracellular domain of TLR3 and inhibit poly(I:C)-induced inflammation. MW: 145.3 KD.
E1134 ABR-238901 ABR-238901 is a novel S100A8/A9 blocker that potently inhibits S100A8/A9 interaction with its receptors RAGE (receptor for advanced glycation endproducts) and TLR4 (toll-like receptor 4).
E0694 Okanin Okanin, a chalcone found in the flower tea Coreopsis tinctoria, effectively reduces LPS-induced microglial activation by inhibiting the TLR4/NF-κB signalling pathways. It also reduces LPS-induced nitric oxide (NO) production and iNOS expression by increasing HO-1 expression. It exhibits a potential as a nutritional preventive measure for neurodegenerative disorders.
S4461 CU-CPT-8m CU-CPT-8m (CPD1578) is a specific antagonist of toll-like receptor 8(TLR8) with IC50 of 67 nM and Kd of 220 nM.
Nat Commun, 2024, 15(1):5678
A2757 Anti-TLR7 Anti-TLR7 is a monoclonal antibody against Toll-like receptor 7 (TLR7) with the potential to treat autoimmune disease. MW: 145.04 KD.
S6719 E6446 dihydrochloride E6446 dihydrochloride is a specific Toll-like receptor 9 inhibitor.
Antioxidants (Basel), 2024, 13(10)1265
A2333 Tomaralimab (Anti-TLR2 / CD282) Tomaralimab (Anti-TLR2 / CD282) is a humanized immunoglobulin (Ig) G4 monoclonal antibody directed against toll-like receptor type 2 (TLR2) with potential anti-inflammatory and antineoplastic activities. It has the potential for research on Myelodysplastic Syndromes (MDS). MW : 145.5 KD.
S9730 CU-CPT9a

CU-CPT9a is a potent and specific antagonist of Toll-like receptor 8 (TLR8) with IC50 of 0.5 nM.

Nat Commun, 2024, 15(1):5678
J Gen Virol, 2023, 104(5)001858
S8133 Resiquimod (R-848) Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. Resiquimod reduces hepatitis C virus (HCV) infection. Phase 2.
Int J Nanomedicine, 2024, 19:3589-3605
Front Immunol, 2024, 15:1331480
Biology (Basel), 2023, 12(2)318
S7161 Motolimod Motolimod is a selective and potent Toll-like receptor 8 (TLR8) agonist with EC50 of 100 nM, > 50-fold selectivity over TLR7. Phase 2.
J Pharmacol Exp Ther, 2024, 388(3):751-764
Cell Rep, 2021, 35(7):109143
J Leukoc Biol, 2020, 1
S7221 Vesatolimod (GS-9620) Vesatolimod (GS-9620) is a potent and selective orally active small molecule agonist of Toll-like receptor 7.
PLoS Pathog, 2022, 18(3):e1010354
J Pharm Biomed Anal, 2020, 179:112987
Stem Cell Res Ther, 2019, 10(1):387
S2979 CU-T12-9 CU-T12-9 is a specific agonist of Toll-like receptor (TLR) 1/2 with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.
Biomedicine & Pharmacotherapy, 2023, 114638
Biomed Pharmacother, 2023, 162:114638
S0494 SM 324405 SM 324405 (compound 9e) is a potent and selective Toll-like receptor 7 (TLR7) agonist with EC50 of 50 nM.
S0078 1V209 (TLR7 agonist T7) 1V209 (T7, TLR7 agonist T7) is an agonist of Toll-like receptor 7 (TLR7) with anti-tumor effects. 1V209 can be used as vaccine adjuvants, enhances antigen specific humoral and cellular immune responses.
S9623 Telratolimod Telratolimod (3M-052, MEDI9197) is an agonist of toll-like receptor 7 (TLR-7) and toll-like receptor 8 (TLR-8) with antitumor activity.
E0639 TLR7/8 agonist 1 dihydrochloride TLR7/8 agonist 1 dihydrochloride is a toll-like receptor TLR7/TLR8 dual-agonistic imidazoquinoline.TLR7/8 agonist 1 retains TLR7-agonistic activity with an EC50 of 20 nM.
S4157 Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).
Nat Commun, 2024, 15(1):1642
Cancer Lett, 2024, 604:217258
Phytomedicine, 2024, 135:156053
S6999 Chloroquine Chloroquine is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.
Signal Transduct Target Ther, 2024, 9(1):65
Mol Cancer, 2024, 23(1):240
Bioact Mater, 2024, 32:277-291
S4430 Hydroxychloroquine (HCQ) Sulfate Hydroxychloroquine (HCQ) Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
Redox Biol, 2024, 75:103274
Phytomedicine, 2024, 10.1016/j.phymed.2023.155152
Breast Cancer Res, 2024, 26(1):33
S7455 Resatorvid (TAK-242) Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 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.
Cancer Cell, 2024, S1535-6108(24)00119-3
Nat Commun, 2024, 15(1):7662
Redox Biol, 2024, 70:103072
S8677 Cu-CPT22 CU-CPT22 shows dose-dependent inhibitory effects blocking Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 ± 0.09 µM while no significant inhibition to TLR2/6. It demonstrates minimal non-specific inhibition against a panel of 10 representative kinases (PDGFRB, MET, DDR2, SRC, MAPK1, PAK1, AKT1, PKC-γ, CAMK1, and PLK4).
Cancer Cell, 2024, S1535-6108(24)00135-1
J Exp Clin Cancer Res, 2023, 42(1):172
J Exp Clin Cancer Res, 2023, 42(1):172
S6597 TLR2-IN-C29 TLR2-IN-C29 (C29) is a Toll-like receptor 2 (TLR2) inhibitor that inhibits TLR2/1 and TLR2/6 signaling.
J Immunother Cancer, 2024, 12(6)e009082
Clin Immunol, 2024, 263:110226
PLoS Pathog, 2024, 20(11):e1012614
S6573 MD2-IN-1 MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD value of 189 μM.
Life Sci Alliance, 2023, 6(3)e202201636
Front Immunol, 2022, 13:995791
Br J Pharmacol, 2021, 10.1111/bph.15412
S3924 Ginsenoside Rb1 Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS.
J Biol Chem, 2024, 300(8):107542
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
J Biol Chem, 2021, S0021-9258(21)00790-0
S8562 IRAK4-IN-2 IRAK4-IN-2 is a reversible kinase inhibitor that modulates IRAK4 function in both the toll-like receptor (TLR) and interleukin 1 receptor (IL-1R) signaling cascades.
Cancer Lett, 2021, 503:75-90
Cancer Lett, 2021, 503:75-90
S0716 E6446 E6446 is an inhibitor of Toll-like receptor (TLR) 7 and 9 signaling in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro.
Cancer Cell, 2024, S1535-6108(24)00135-1
Front Immunol, 2024, 15:1354055
JCI Insight, 2023, 8(22)e171054
S9234 Schaftoside Schaftoside, a bioactive compound found in the Herba Desmodii Styracifolii, exhibits pancreatic lipase inhibitory activity. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission.
S6934 AMG-9810 AMG-9810 is a potent, competitive and selective vanilloid receptor 1 (TRPV1) antagonist and inhibits capsaicin activation with IC50 of 24.5 nM and 85.6 nM for human TRPV1 and rat TRPV1, repectively. AMG-9810 blocks all known modes of TRPV1 activation, including protons-, heat-, and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG-9810 significantly reduces the mRNA expression of TLR2 and TLR4. AMG-9810 also promotes mouse skin tumorigenesis mediated through EGFR/Akt/mTOR signaling.
S9931 Enpatoran Hydrochloride Enpatoran (M5049) hydrochloride is a potent, orally active, and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM, respectively, in HEK293 cells.
S0139 MD2-TLR4-IN-1 MD2-TLR4-IN-1 (Compound 22m) is a potent inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4). MD2-TLR4-IN-1 (compound 22m) inhibits lipopolysaccharide (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 of 0.89 μM and 0.53 μM, respectively.
E1134 ABR-238901 ABR-238901 is a novel S100A8/A9 blocker that potently inhibits S100A8/A9 interaction with its receptors RAGE (receptor for advanced glycation endproducts) and TLR4 (toll-like receptor 4).
E0694 Okanin Okanin, a chalcone found in the flower tea Coreopsis tinctoria, effectively reduces LPS-induced microglial activation by inhibiting the TLR4/NF-κB signalling pathways. It also reduces LPS-induced nitric oxide (NO) production and iNOS expression by increasing HO-1 expression. It exhibits a potential as a nutritional preventive measure for neurodegenerative disorders.
S6719 E6446 dihydrochloride E6446 dihydrochloride is a specific Toll-like receptor 9 inhibitor.
Antioxidants (Basel), 2024, 13(10)1265
A2696 Anti-TLR3 / CD283 (CNTO5429) Anti-TLR3 / CD283 (CNTO5429) is a novel antibody that binds to the extracellular domain of TLR3 and inhibit poly(I:C)-induced inflammation. MW: 145.3 KD.
A2757 Anti-TLR7 Anti-TLR7 is a monoclonal antibody against Toll-like receptor 7 (TLR7) with the potential to treat autoimmune disease. MW: 145.04 KD.
A2333 Tomaralimab (Anti-TLR2 / CD282) Tomaralimab (Anti-TLR2 / CD282) is a humanized immunoglobulin (Ig) G4 monoclonal antibody directed against toll-like receptor type 2 (TLR2) with potential anti-inflammatory and antineoplastic activities. It has the potential for research on Myelodysplastic Syndromes (MDS). MW : 145.5 KD.
S7850 Lipopolysaccharides Lipopolysaccharides (LPSs, Endotoxin,LPS) is an endotoxin derived from the outer leaflet of the outer membrane of Gram-negative bacteria. Lipopolysaccharides consists of an antigen O-specific chain, a core oligosaccharide and lipid A. Lipopolysaccharides is a pathogenic associated molecular pattern (PAMP) that activates the immune system. Lipopolysaccharides activates TLR-4 on immune cells. Lipopolysaccharides induces secretion of cell migrasome.
Int Immunopharmacol, 2024, 137:112426
Biomolecules, 2024, 14(7)741
Sci Rep, 2024, 14(1):13102
S9937 CU-CPD107 CU-CPD107 is a selective, dual-activity small-molecule which demonstrated differential activity against the TLR8 agonists and ssRNA ligands. In the presence of R848, CU-CPD107 acts as a TLR8 signaling inhibitor (IC50=13.7 μM). In the presence of ssRNA, CU-CPD107 shows synergistic agonist activities, while CU-CPD107 alone is unable to influence TLR8 signaling.
S0822 TLR4-IN-C34 TLR4-IN-C34 (TLR4-C34, C34, TLR4-C34-IN) is a potent and selective antagonist of Toll-like receptor 4 (TLR4). TLR4-IN-C34 reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.
Exp Mol Med, 2024, 56(2):408-421.
J Immunother Cancer, 2024, 12(6)e009082
Am J Physiol Gastrointest Liver Physiol, 2024, 327(6):G741-G753
S0002 IAXO-102 IAXO-102 is an antagonist of TLR4 targeting both MD-2 and CD14 co-receptors. IAXO-102 inhibits MAPK and p65 NF-κB phosphorylation and downregulates the expression of TLR4 dependent proinflammatory proteins. IAXO-102 inhibits experimental abdominal aortic aneurysm (AAA) development.
S4461 CU-CPT-8m CU-CPT-8m (CPD1578) is a specific antagonist of toll-like receptor 8(TLR8) with IC50 of 67 nM and Kd of 220 nM.
Nat Commun, 2024, 15(1):5678
S9730 CU-CPT9a

CU-CPT9a is a potent and specific antagonist of Toll-like receptor 8 (TLR8) with IC50 of 0.5 nM.

Nat Commun, 2024, 15(1):5678
J Gen Virol, 2023, 104(5)001858
S8133 Resiquimod (R-848) Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. Resiquimod reduces hepatitis C virus (HCV) infection. Phase 2.
Int J Nanomedicine, 2024, 19:3589-3605
Front Immunol, 2024, 15:1331480
Biology (Basel), 2023, 12(2)318
S7161 Motolimod Motolimod is a selective and potent Toll-like receptor 8 (TLR8) agonist with EC50 of 100 nM, > 50-fold selectivity over TLR7. Phase 2.
J Pharmacol Exp Ther, 2024, 388(3):751-764
Cell Rep, 2021, 35(7):109143
J Leukoc Biol, 2020, 1
S7221 Vesatolimod (GS-9620) Vesatolimod (GS-9620) is a potent and selective orally active small molecule agonist of Toll-like receptor 7.
PLoS Pathog, 2022, 18(3):e1010354
J Pharm Biomed Anal, 2020, 179:112987
Stem Cell Res Ther, 2019, 10(1):387
S2979 CU-T12-9 CU-T12-9 is a specific agonist of Toll-like receptor (TLR) 1/2 with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.
Biomedicine & Pharmacotherapy, 2023, 114638
Biomed Pharmacother, 2023, 162:114638
S0494 SM 324405 SM 324405 (compound 9e) is a potent and selective Toll-like receptor 7 (TLR7) agonist with EC50 of 50 nM.
S0078 1V209 (TLR7 agonist T7) 1V209 (T7, TLR7 agonist T7) is an agonist of Toll-like receptor 7 (TLR7) with anti-tumor effects. 1V209 can be used as vaccine adjuvants, enhances antigen specific humoral and cellular immune responses.
S9623 Telratolimod Telratolimod (3M-052, MEDI9197) is an agonist of toll-like receptor 7 (TLR-7) and toll-like receptor 8 (TLR-8) with antitumor activity.
E0639 TLR7/8 agonist 1 dihydrochloride TLR7/8 agonist 1 dihydrochloride is a toll-like receptor TLR7/TLR8 dual-agonistic imidazoquinoline.TLR7/8 agonist 1 retains TLR7-agonistic activity with an EC50 of 20 nM.

TLR阻害剤の選択性比較

Tags: TLR inhibitor|TLR agonist|TLR activator|TLR inducer|TLR antagonist|TLR signaling pathway|TLR assay kit