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| 品牌 | absin | CAS | 217645-70-0 |
|---|---|---|---|
| 分子式 | C21H24ClFN4O3 | 纯度 | 98% |
| 分子量 | 434.89 | 货号 | abs47028017 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | is a potent | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
BX-471 217645-70-0
| 产品描述 | |
| 描述 | BX471 is a potent, selective non-peptide CCR1 antagonist (Ki = 1 nM for human CCR1); exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4. |
| 纯度 | 98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 可溶性/溶解性 | DMSO >51 mg/ml |
| 生物活性 | |
| 靶点 | CCR |
| In vitro(体外研究) | BX471 is a potent functional antagonist based on its ability to inhibit a number of CCR1-mediated effects including Ca2+ 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 125I-MIP-1α/CCL3 binding to mouse CCR1 in a concentration-dependent manner with a Ki of 215±46 nM. Increasing concentrations of BX471 inhibits the Ca2+ transients induced by MIP-1α/CCL3 in both human and mouse CCR1 with IC50 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. |
| In vivo(体内研究) | 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. |
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| 研究领域 | |
| 研究领域 | Immunology NeuroscienceEndocrine system Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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