网站主页 >> CAS数据库列表 >> (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
(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
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- CAS号:
- 217645-70-0
- 英文名:
- Urea, N-[5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)Methyl]-2-Methyl-1-piperazinyl]-2-oxoethoxy]phenyl]-
- 英文别名:
- CS-1299;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;BX471,ZK811752,CCR,CC chemokine receptor,Inhibitor,inhibit,ZK 811752;(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
- 中文名:
- (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
- 中文别名:
- 化合物BX-471;BX 471,CCR1拮抗剂;(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
- CBNumber:
- CB72628515
- 分子式:
- C21H24ClFN4O3
- 分子量:
- 434.89
- MOL File:
- 217645-70-0.mol
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(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)脲化学性质
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沸点:
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593.5±50.0 °C(Predicted)
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密度:
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1.346±0.06 g/cm3(Predicted)
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储存条件:
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Inert atmosphere,2-8°C
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溶解度:
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DMSO: ≥25mg/mL
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酸度系数(pKa):
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13.66±0.70(Predicted)
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形态:
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White powder
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颜色:
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white to tan
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(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)脲性质、用途与生产工艺
BX471 (ZK-811752) 是以一种口服有效的，选择性，非多肽的 CCR1 拮抗剂，Ki 值为 1 nM，对其选择性是对 CCR2，CCR5 和 CXCR4 的 250 倍。
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MIP-1α-CCR1
1 nM (Ki)
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RANTES-CCR1
2.8 nM (Ki)
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MCP-3-CCR1
5.5 nM (Ki)
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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.
(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
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/16 | B6060 | BX 471
BX 471 | 217645-70-0 | 5mg | 295元 |
| 2024/01/16 | B6060 | BX 471
BX 471 | 217645-70-0 | 25mg | 1080元 |
(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
生产厂家
217645-70-0, (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 相关搜索:
- Inhibitors
- 合成有机化合物配体
- 生物试剂
- 抑制剂
- 小分子抑制剂
- 小分子抑制剂，天然产物
- C21H24ClFN4O3
- BX 471,CCR1拮抗剂
- 化合物BX-471
- (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
- (2R)-1-[[[4-氯-2-(脲基)苯氧基]甲基]羰基]-2-甲基-4-(4-氟苄基)哌嗪
- 217645-70-0
- 1-[(4-chloro-2-ureido-phenoxy-)methyl-carbonyl-]-2-(R)-methyl-4-(4-fluoro-benz-yl)-piperidine
- BX471,ZK811752,CCR,CC chemokine receptor,Inhibitor,inhibit,ZK 811752
- (R)-1-[5-Chloro-2-[2-[4-(4-fluorobenzyl)-2-methylpiperazin-1-yl]-2-oxoethoxy]phenyl]urea
- ZK-811752(BX-471) (free base)
- (2R)-1-[[2-[(Aminocarbonyl)amino]-4-chlorophenoxy]acetyl]-4-[(4-fluorophenyl)methyl]-2-methylpiperazine
- BX471 - CAS 217645-70-0 - Calbiochem
- ZK 811752;ZK811752;ZK-811752;BX-471; BX 471;BX-471
- BX-471(Free base)
- CS-1299
- (2R)-1-[[[4-Chloro-2-(ureido)phenoxy]methyl]carbonyl]-2-methyl-4-(4-fluorobenzyl)piperazine
- Piperazine,1-[[2-[(aminocarbonyl)amino]-4-chlorophenoxy]acetyl]-4-[(4-fluorophenyl)methyl]-2-methyl-, (2R)-
- BX471(ZK-811752)
- N-[5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)methyl]-2-methyl-1-piperazinyl]-2-oxoethoxy]phenyl]-urea
- (2R)-1-[[2-[(Aminocarbonyl)amino]-4-chlorophenoxy]acetyl]-4-[(4-fluorophenyl)methyl]-2-methylpiperazine ZK811752 (BX471)
- ZK811752 (BX471)
- (5-Chloro-2-{2-[4-(4-fluoro-benzyl)-2-Methyl-piperazin-1-yl]-2-oxo-ethoxy}-phenyl)-urea
- Urea, N-[5-chloro-2-[2-[(2R)-4-[(4-fluorophenyl)Methyl]-2-Methyl-1-piperazinyl]-2-oxoethoxy]phenyl]-