产品说明书
Plerixafor octaHCl
 |
同义名 : | AMD3100 octahydrochloride;JM3100 octahydrochloride;Plerixafor 8HCl;SID791 octahydrochloride;Plerixafor octahydrochloride |
| CAS号 : | 155148-31-5 | |
| 货号 : | A268315 | |
| 分子式 : | C28H62Cl8N8 | |
| 纯度 : | 98% | |
| 分子量 : | 794.47 | |
| MDL号 : | MFCD04974488 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
H2O: 100 mg/mL(125.87 mM)，配合低频超声助溶 |
|
| 动物实验配方： |
PO 0.5% CMC-Na 80 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 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 inflammation or infection sites and implicated in several immuno-related disease states, organogenesis, angiogenesis and tumor growth and metastasis. Plerixafor Octahydrochloride is the hydrochloride form of AMD3100. 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 | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.26mL 0.25mL 0.13mL |
6.29mL 1.26mL 0.63mL |
12.59mL 2.52mL 1.26mL |
