tlr2 antagonist-1

TLR2antagonist-1 is a selective antagonist of Toll-like receptor 2 (TLR2). It effectively inhibits excessive activation of TLR2, with an IC50 value of 11.41 μM, and reduces the production of inflammatory factors. TLR2antagonist-1 exhibits metabolic stability, with a half-life (T1/2) of 16.67 minutes in mouse liver microsomes. This compound is useful for research in inflammation, immunology, and neurological disorders.

MMG-11 inhibits both TLR2/1 and TLR2/6 signaling (IC50s: 1.7 μM for Pam3CSK4-induced hTLR2/1 and 5.7 μM for Pam2CSK4-induced hTLR2/6 responses). MMG-11 is an effective and selective human TLR2 antagonist with low cytotoxicity.

MMG-11 quarterhydrate is a potent and selective antagonist of human TLR2, inhibiting both TLR2/1 and TLR2/6 signaling with low cytotoxicity. The IC50 values for Pam3CSK4-induced hTLR2/1 and Pam2CSK4-induced hTLR2/6 responses are 1.7 μM and 5.7 μM, respectively [1].

NCI 126224 is a Toll-like receptor 4 (TLR4) antagonist that selectively inhibits nitric oxide production induced by the TLR4 agonist LPS in RAW 264.7 macrophages (IC50 = 0.31 µM), while exhibiting weaker effects against the TLR7/8 agonist R-848, TLR1/2 agonist Pam3CSK4, and TLR3 agonist poly(I:C). NCI 126224 also inhibits FSL-1-induced NO production at 0.6 µM and suppresses LPS-induced NF-κB activity in BV-2 glial cells, while reducing IL-1β and TNF-α levels in RAW 264.7 cells (IC50s of 5.92 and 1.54 µM, respectively). 0.42, and 1.54 µM, respectively), demonstrating its significant value in studies of inflammatory and innate immune signaling pathways.