TLR

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.

Resatorvid (TAK-242), a selective Toll-like receptor 4 (TLR4) inhibitor, binds directly to Cys747 to prevent TLR4-TIRAP interaction, thereby blocking downstream signaling. Resatorvid exhibits antitumor, anti-inflammatory, and neuroprotective activities.

Pam3CSK4 TFA (Pam3Cys-Ser-(Lys)4 TFA) is a Toll-like receptor 1 2 agonist with EC50 of 0.47 ng mL for human TLR1 2.

Flavone glycoside from Robinia with antibacterial and diuretic properties; derived from kaempferol.The ability of robinin to reverse the multidrug resistance of the human colon cancer cell line Colo 320 expreβing MDR1 LRP was explored by monitoring their uptake of Rhodamine 123, but was shown to have minimal effect. Robinin (NSC-9222) was detected in lysates of the human breast cancer cell line MCF-7 using liquid chromatography-tandem maβ spectrometry.

Procyanidin B1, isolated from commonly eaten fruits, binds to the TLR4 MD-2 complex and has anti-inflammatory activity.

Afimetoran (BMS-986256) is a toll-like receptor antagonist. Afimetoran can be used in the research of inflammatory and autoimmune diseases.

Polyinosinic-polycytidylic acid (Poly(I:C)) is a double-stranded RNA (dsRNA) and a TLR3 agonist. Polyinosinic-polycytidylic acid induces natural immunity in mammals.

CL264, a selective agonist of TLR7, can be used in studies about innate immune signals.

TLR7 8-IN-1, a crystalline TLR7 TLR8 inhibitor from patent WO2019220390 (compound 2b), is a valuable compound for autoimmune disease research.

Resiquimod (R848) is a Toll-like receptor 7 8 (TLR7 TLR8) agonist that induces cytokine upregulation. Resiquimod is an immunomodulator with antitumor and antiviral activity.

Telratolimod (MEDI9197) is a toll-like receptors 7 8 agonist. It has an antitumor activity.

Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) 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).

Corilagin has anti-inflammatory activity. Corilagin has a significant antitumour potential and lower toxicity in normal cells in vitro.Corilagin can enhance the cytotoxicity of both cisplatin and doxorubicin on the Hep3B hepatoma cells.Corilagin has antiviral activity, reduces the cytotoxicity induced by EV71 or CA16 on Vero cells with and IC50 value of 5.6 and 32.33 μg mL, respectively. Corilagin shows the potential to protect against HSV-1-induced encephalitis, and the beneficial effects may be mediated by inhibiting TLR2 signaling pathways.Corilagin has antifibrotics property and is potentiated in treating idiopathic pulmonary fibrosis(IPF), attenuates bleomycin-induced epithelial injury and fibrosis via inactivation of oxidative stress, proinflammatory cytokine release and NF-κB and TGF-β1 signaling. Solvent:Pyridine, Methanol, Ethanol, etc.

ODN 1668 is an immunostimulatory class B CpG oligodeoxynucleotide (ODN) containing an intact thio backbone of one or more CpG dinucleotides, which is primarily used as an agonist for Toll-like receptor 9 (TLR9), and also upregulates the level of IgM and induces an antimicrobial immune response via a CaTLR9-dependent pathway.

Enpatoran hydrochloride (M5049 hydrochloride) is an orally active, selective, and potent TLR7 8 inhibitor with antiviral activity for the study of autoimmune diseases and COVID-19 pneumonia.

Sparstolonin B, a selective TLR2 and TLR4 antagonist, is an isocoumarin compound isolated from the tubers of Sparganium stoloniferum and Scirpus yagara with anti-HIV, anticancer, antitumour and anti-inflammatory activities, inhibits selective Toll-like receptors, inhibits free fatty acids It inhibits selective Toll-like receptors, inhibits free fatty acid palmitate-induced chondrocyte inflammation and attenuates post-traumatic arthritis in obese mice, and inhibits lipopolysaccharide-induced inflammation in 3T3-L1 adipocytes, which can be used for validation and mammary carcinoma studies.

Schaftoside (APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE) has antioxidant and anticancer activity.

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).

TLR4-IN-C34 is an inhibitor of TLR4, and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis

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.

Imiquimod hydrochloride (R 837 hydrochloride), a selective toll-like receptor 7 (TLR7) agonist, functions as an immune response modifier with in vivo antiviral and antitumor properties, and is utilized in researching external genital and perianal warts, cancer, and COVID-19 [1] [2].

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.

A natural, noncaloric sweetener with a potency 300 times more than that of regular sucrose. Exhibits transepithelial p-aminohippurate transport via organic anion transport system interference.

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.