217645-70-0
![217645-70-0 结构式](/CAS/GIF/217645-70-0.gif)
基本信息
(2R)-1-[[[4-氯-2-(脲基)苯氧基]甲基]羰基]-2-甲基-4-(4-氟苄基)哌嗪
(R)-1-[5-氯-2-[2-[4-(4-氟苄基)-2-甲基哌嗪-1-基]-2-氧代乙氧基]苯基]脲
BX471(ZK-811752)
ZK811752 (BX471)
BX-471(Free base)
ZK-811752(BX-471) (free base)
BX471 - CAS 217645-70-0 - Calbiochem
ZK 811752
ZK811752
ZK-811752
BX-471
BX 471
BX-471
(5-Chloro-2-{2-[4-(4-fluoro-benzyl)-2-Methyl-piperazin-1-yl]-2-oxo-ethoxy}-phenyl)-urea
(R)-1-[5-Chloro-2-[2-[4-(4-fluorobenzyl)-2-methylpiperazin-1-yl]-2-oxoethoxy]phenyl]urea
(2R)-1-[[[4-Chloro-2-(ureido)phenoxy]methyl]carbonyl]-2-methyl-4-(4-fluorobenzyl)piperazine
物理化学性质
报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
2024/08/19 | B6060 | BX 471 BX 471 | 217645-70-0 | 5mg | 295元 |
2024/08/19 | B6060 | BX 471 BX 471 | 217645-70-0 | 25mg | 1080元 |
常见问题列表
MIP-1α-CCR1 1 nM (Ki) |
RANTES-CCR1 2.8 nM (Ki) |
MCP-3-CCR1 5.5 nM (Ki) |
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.
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.