BX471 hydrochloride is a potent, selective, orally available CCR1 antagonist with Ki of 1 nM for hCCR1, displays 100 times less affinity for rat CCR1.
BX471 shows 10,000-fold selectivity for CCR1 compared with 28 GPCRs.
BX471 displays CCR1 ligands MIP-1α, RANTES, and MCP-3 with high affinity (Ki=1-5.5 nM), inhibits a number of CCR1-mediated effects including Ca(2+) mobilization, increase in extracellular acidification rate, CD11b expression.
BX471 effectively reduces disease in a rat experimental allergic encephalomyelitis model of multiple sclerosis.
