Enpatoran (M5049) is an orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran can block both innate and adaptive autoimmunity. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran (M5049) can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran (M5049) inhibits cytokine release, causing great potency in pharmacokinetic/pharmacodynamic properties.

TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride (compound 9) is a drug-linker conjugate for ADC with potent antitumor activity by using TLR7/8 agonist 4, linked via the cleavable ADC linker hydroxy-PEG10-acid.

Gardiquimod trifluoroacetate is a specific TLR7 agonist which can also inhibit HIV-1 reverse transcriptase.

Imiquimod hydrochloride (R 837 hydrochloride), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod hydrochloride exhibits antiviral and antitumor effects in vivo. Imiquimod hydrochloride can be used for the research of external genital, perianal warts, cancer and COVID-19.

Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling.

1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects. 1V209 can be conjugated with various polysaccharides to improve its water solubility, and enhance its efficacy, and maintain low toxicity.

GS-9620 is a potent and selective orally active small molecule agonist of Toll-like receptor 7(TLR-7) in chimpanzees with chronic HBV infection.

Motolimod (VTX-2337) is a novel TLR8 agonist that activates NK cells and augments ADCC.

TLR4-IN-C34-C2-COO is a linker that incorporates TLR4 inhibitor TLR4-IN-C34. TLR4-IN-C34 inhibits TLR4 in enterocytes and macrophages, and reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.

TLR7/8 agonist 3 is a potent TLR7 and TLR8 agonist, extracted from patent US20170114137A1.

TLR7/8 agonist 1 is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.

Telratolimod (MEDI 9197, 3M 052) is a novel, injectable, tissue-retained TLR7/8 agonist that forms a tissue depot with gradual, sustained release, allowing local TLR triggering activity without systemic cytokine release.

SMU127 (SMU-127, ZINC666243) is a specific TLR1-TLR2 small molecule agonist with EC50 of 0.55 uM.

A potent TLR7/8 agonist that induces robust production of the Th1-polarizing cytokines TNF-alpha and IL-12 from neonatal antigen-presenting cells (APCs)..

3M-011 is a potent TLR7/8 agonist and cytokine inducer; stimulates type I interferon (IFN) and other cytokines such as TNF-alpha, IL-12, and IFN-gamma from rat peripheral blood mononuclear cells; induces IL-12 and COX-2 expression in mDC from HIV+ and HIV- individuals, and inhibits H3N2 influenza viral replication in the nasal cavity; potentiates NK cytotoxicity, and shows antitumor effects in scid/B6 mice and scid/NOD mice.

A selective TLR8 agonist that induces activation of NF-κB at 0.4 uM.

ANA975 is an oral prodrug of the TLR-7 agonist Isatoribine (ANA245.

CU115 is a potent TLR8 antagonist (IC50=1.04 µM), and shows selective for TLR8 over TLR7 (IC50=>50 µM). CU 115 decreases TNF-α and IL-1β production activated by R-848 in THP-1 cells.

Novel TLR7 agonist via immune response induction and tumor microenvironment modulation

Toll-like receptor 2/6 (TLR-2/6) agonist, regulating Lcn2 gene, promoting collateral growth

Novel anticryptosporidial agent, acting as a toll-like receptor-2 (TLR2) antagonist

Novel potent TLR1/2 Specific Agonist, Suppressing Leukemia Cancer Cell Growth by Stimulating Cytotoxic T Lymphocytes

E6742 (E6742) is a potent, selective, dual TLR7/8 inhibitor with binding Kd of 1.7 uM/37 nM in ITC assays, respectively, inhibits TLR7/8 agonist CL097 induced reporter activation with IC50 values of 22, 68, and 3.0 nM for hTLR7, mTLR7, and hTLR8, respecti

CL097, a potent TLR7/8 agonist, induces pro-inflammatory cytokines in macrophages. CL097 induces NADPH oxidase priming, resulting in an increase of the fMLF-stimulated ROS production.

RS 09 is a TLR4 agonist. RS 09 promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. RS 09 acts as an adjuvant in vivo; RS 09 enhances X-15 specific antibody serum concentrations, when administered with X-15-KLH in mice.

AZ617 is a potent TLR4 agonist.

TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis[1][2].

Gardiquimod is a TLR7 agonist, inducing the activation of NF-B in HEK293 cells expressing human or mouse TLR7.

Paquinimod is a S100A9 inhibitor, which prevents S100A9 binding to TLR-4.

TJ-M2010-5 is a MyD88 inhibitor that binds to the TIR domain of MyD88 to interfere with its homodimerization, and the TLR/MyD88 signal pathway. TJ-M2010-5 can be used for the research of myocardial ischemia/reperfusion injury (MIRI).