CS-1298
中文名称 | CS-1298 |
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中文同义词 | BX471盐酸盐;化合物 T14845;(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 盐酸盐 |
英文名称 | BX471 (hydrochloride) |
英文同义词 | BX471 (hydrochloride);N-[5-Chloro-2-[2-[4-(4-fluorobenzyl)-2(R)-methylpiperazin-1-yl]-2-oxoethoxy]phenyl]urea hydrochloride ZK-811752(BX471);CS-1298;BX471 HYDROCHLORIDE;BX-471 HYDROCHLORIDE;BX 471 HYDROCHLORIDE;ZK-811752 hydrochloride;(R)-1-(5-Chloro-2-(2-(4-(4-fluorobenzyl)-2-methylpiperazin-1-yl)-2-oxoethoxy)phenyl)urea hydrochloride |
CAS号 | 288262-96-4 |
分子式 | C21H25Cl2FN4O3 |
分子量 | 471.35 |
EINECS号 | |
相关类别 | |
Mol文件 | 288262-96-4.mol |
结构式 | ![]() |
CS-1298 性质
储存条件 | under inert gas (nitrogen or Argon) at 2-8°C |
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溶解度 | 二甲基亚砜:150 mg/ml(318.23 mM) |
形态 | 固体 |
颜色 | 白色至黄色 |
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-12080A | BX471 hydrochloride | 5 mg | 1025元 | |
2024/08/19 | HY-12080A | CS-1298 BX471 hydrochloride | 288262-96-4 | 10mg | 1640元 |