BX-471

bx471是一种有效的、选择性的CCR1拮抗剂。BX471 is a potent functional antagonist based on its ability to inhibit a number of CCR1-mediated effects including Ca²⁺ mobilization, increase in extracellular acidification rate, CD11b expression, and leukocyte migration. BX471 demonstrats a greater than 10,000-fold selectivity for CCR1 compared with 28 G-protein-coupled receptors^[1]. BX471 is also able to displace ¹²⁵I-MIP-1α/CCL3 binding to mouse CCR1 in a concentration-dependent manner with a K_i of 215±46 nM. Increasing concentrations of BX471 inhibits the Ca²⁺ transients induced by MIP-1α/CCL3 in both human and mouse CCR1 with IC₅₀ of 5.8±1 nM and 198±7 nM, respectively^[2]. BX471 (0.1-10 μM) shows a dose-dependent inhibition of RANTES-mediated and shear-resistant adhesion on IL-1β-activated microvascular endothelium in shear flow in isolated blood monocytes. BX471 also inhibits the RANTES-mediated adhesion of T lymphocytes to activated endothelium