BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with K i of 1 nM for human CCR1 , and exhibits 250-fold selectivity for CCR1 over CCR2 , CCR5 and CXCR4 . In Vitro BX471 is a potent functional antagonist based on its ability to inhibit a number of CCR1-mediated effects including Ca 2+ 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. BX471 is also able to displace 125 I-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 Ca 2+ transients induced by MIP-1α/CCL3 in both human and mouse CCR1 with IC 50 of 5.8±1 nM and 198±7 nM, respectively. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo BX471 (4 mg/kg, p.o. or i.v.) is orally active with a bioavailability of 60% in dogs. Furthermore, BX471 effectively reduces disease in a rat experimental allergic encephalomyelitis model of multiple sclerosis . BX471 (20 mg/kg, s.c.) reaches peak plasma levels of 9 μM by around 30 minutes, and this rapidly declines to approximately 0.4 μM after 2 hours. From 4 to 8 hours the drug plasma levels drops to 0.1 μM or lower. Mice treated with 20 mg/kg of BX471 for 10 days shows a reduction of interstitial CD45 positive leukocytes of approximately 55%. BX471 has a borderline significant effect on the number of CCR5-positive CD8 cells in the peripheral blood. BX471 reduces the amount of FSP1-positive cells by 65% in UUO kidneys as compared with vehicle control. Pretreatment witih BX471 reduces macrophage and neutrophil accumulation in kidney after ischemia-reperfusion injury. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:MIP-1α-CCR1 1 nM (Ki) RANTES-CCR1 2.8 nM (Ki) MCP-3-CCR1 5.5 nM (Ki)
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BX471 hydrochloride
CAS number：288262-96-4 molecular formula：C21H25Cl2FN4O3
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| Chinese alias | BX471盐酸盐 | ||
| English alias | BTK'168 | BX471hydrochloride | Urea, N-(5-chloro-2-(2-((2R)-4-((4-fluorophenyl)methyl)-2-methyl-1- Piperazinyl)-2-oxoethoxy)phenyl)-, hydrochloride (1:1) | BX471 hydrochloride | ZK811752 | ZK-811752 | s8926 | (R)-1-(5-Chloro-2-(2-(4-(4-fluorobenzyl)-2 | ||
| CAS number | 288262-96-4 | molecular formula | C21H25Cl2FN4O3 |
| molecular weight | 471.3 g/mol | Exact mass | ≥99% |
| PSA | 87.900 Ų | logp | - |
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