AXC-715 trihydrochloride is a TLR7/TLR8 dual agonist, extracted from patent WO2020168017 A1. AXC-715 trihydrochloride, compound D from WO2020190734A1, can be used for synthesis of antibody-adjuvant immunoconjugates, comprising an antibody construct that binds programmed death-ligand 1 (PD-L1) linked to one or more adjuvants.
TAK-242 (Resatorvid), a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, inhibits the production of lipopolysaccharide-induced inflammatory mediators by binding to the intracellular domain of TLR4.
SMU-14a is a TLR3 inhibitor (IC50: 0.18 µM). SMU-14a inhibits IL-6 secretion in mouse peritoneal macrophages and downregulates TNF-α in human peripheral blood monocytes. SMU-14a exerts anti-inflammatory effects by reducing the phosphorylation of p65, ERK, and TBK1 through NF-κB, MAPK, and IRF3 signaling pathways, and decreasing serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels. SMU-14a can be used in the study of acute hepatitis.
Pixatimod free acid (PG545 free acid) is a mimetic of Heparan Sulfate. 17β-Hydroxy exemestane is an aromatase inhibitor (IC50 = 69 nM) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC50= 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats.
FGT-4 is a folate receptor β (FR-β) targeting chimeric molecule. FGT-4 is a TLR7 agonist. FGT-4 facilitates the secretion of iNOS and proinflammatory cytokine IL-6 associated with M1 macrophages and enhances the proliferation of cytotoxic CD8+ T cells. FGT-4 has anti-tumor activity in the 4T1 breast cancer mouse model. FGT-4 can be used for the study of cancer immunity.
Creatine ethyl ester (CEE) is a readily available form of creatine used in supplements. Creatine ethyl ester (CEE) upregulates TLRs (TLR2, 3, 4 and TLR7) over the short-term.