molecules of the month

“compound 7f” is an antagonist of the endosomal TLRs 7/8/9, which induce inflammation in response to internalized single-stranded RNA or hypomethylated double-stranded DNA. Potency and selectivity within endosomal TLR’s (3, 7, 8, 9) and against cell-surface TLR’s (1, 2, 4, 5, 6) has been difficult to achieve. Compound 7f has single-digit nanomolar activity against TLRs 7 and 8 in human whole blood, and submicromolar activity against TLR9. Its oral bioavailability in rodents makes it a useful tool compound for studying TLR antagonism in different disease models.