产品说明书
Plerixafor
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同义名 : | AMD 3100;JM3100;JKL 169;Mozobil;SDZ SID 791;SID791 |
| CAS号 : | 110078-46-1 | |
| 货号 : | A195007 | |
| 分子式 : | C28H54N8 | |
| 纯度 : | 99% | |
| 分子量 : | 502.78 | |
| MDL号 : | MFCD05662218 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 1.5 mg/mL(2.98 mM)，配合低频超声，水浴加热至45℃，并调节pH至5，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO 无水乙醇: 45 mg/mL(89.5 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇 |
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| 动物实验配方： |
PO 0.5% CMC-Na 30 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | Through binding with CC- and CXC-chemokines, CCR and CXCR, the subsets of the chemokine receptor family can trigger an intracellular signal transduction cascade, thus mediating the recruitment of immune cells to the in£ammation or infection sites and implicated in several immuno-related disease states, organogenesis, angiogenesis and tumor growth and metastasis. AMD3100 is a selective antagonist of CXCR4 with IC50 values ranging in 0.01-0.13μg/ml for antagonizing SDF-1, but not itself, activated calcium flux in different cells tested, including CXCR4-transfected U87 and CD4 cells, freshly isolated PBMCs, SupT1, THP-1, HSB-2, Molt-4 and L1210 cells. The inhibitory effect of AMD3100 against the induced endocytosis of CXCR4 is selectively SDF-1-dependent but not phorbol ester. Pre-incubated with AMD3100 at concentration of 0.04, 0.2, 1, 5 and 25μg/ml could dose-dependently inhibit the SDF-1-induced (200 ng/ml) chemotaxis of human PBMCs[1]. In vivo study showed that intraperitoneal injection with 5mg/kg AMD3100 can alter the potential of mesenchymal stem cells mobilization induced by different growth factors, including IGF-1, SCF, PDGF and VEGF, in mice, which may be mediated through Akt/PI3K, MEK1/2-Erk1/2 and smad2/3 as key signaling pathways[2]. | ||
| 作用机制 | Not found | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| CEM-SS cells | Function assay | Effective concentration of compound against HIV-1 LAI strain in CEM-SS cells, EC50=127 nM | 14698189 | ||
| CHOK1 cells | Function assay | Displacement of [125I]SDF1alpha from CXCR4 expressed in CHOK1 cells, IC50=0.81 nM | 17715128 | ||
| GHOST CXCR4 cell line | Function assay | Inhibitory concentration of compound against HIV-1 LAI strain in GHOST CXCR4 cell line, IC50=0.95 nM | 14698189 | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01164475 | - | Completed | - | - | |
| NCT01711073 | End Stage Liver DIsease | Phase 1 | Unknown | September 2013 | United States, New Jersey ... 展开 >> University of Medicine and Dentistry of New Jersey Recruiting Newark, New Jersey, United States, 07101 Contact: Baburao Koneru, MD koneruba@umdnj.edu 收起 << |
| NCT01123499 | - | Recruiting | - | United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Recruiting Bethesda, Maryland, United States, 20892 Contact: Sandra Maxwell, B.S.N. 301-402-1773 maxwells@niaid.nih.gov 收起 << | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.99mL 0.40mL 0.20mL |
9.94mL 1.99mL 0.99mL |
19.89mL 3.98mL 1.99mL |
| 参考文献 |
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