生物活性
Plerixafor八盐酸盐是CXCR4趋化因子受体拮抗剂，对于CXCR4和CXCL12调节的趋化作用 IC50分别为44 nM和5.7 nM。Plerixafor 8HCl (AMD3100 8HCl)也抑制SDF-1/CXCL12 配体结合，IC50为 651 nM。Plerixafor 8HCl (AMD3100 8HCl)抑制 SDF-1调节的GTP结合, SDF-1 调节的钙流，和 SDF-1调节的趋化性，IC50分别为27 nM, 572 nM 和51 nM。Plerixafor 8HCl (AMD3100 8HCl)作用于表达多种GPCRs，包括CXCR4,CCR4 和 CCR7的CCRF-CEM细胞，不会有的钙流。Plerixafor通过提高细胞因子产量，调动骨髓EPCs, 和增强成纤维细胞和单核细胞/巨噬细胞的活性,因此提高血管生成，而促进糖尿病小鼠伤口愈合。
化学数据
| 分子量 | 794.47 |
| 分子式 | C28H54N8.8HCl |
| CAS号 | 155148-31-5 |
| 纯度 | >98% |
| 溶解性（25°C） | Water 100 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | OS cell lines (LM8 and Dunn) |
| 方法 | MTT assay.
The effects of CXCL12 and AMD3100 on the survival of two OS cell lines (LM8 and Dunn) were assessed using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cells were seeded in 96-well plates at 2×103/well in DMEM-h. After overnight growth, the cells were cultured for 7 days in FBS-free medium in the presence of 0 or 100 ng/ml CXCL12, 30 μM AMD3100 alone or 100 ng/ml CXCL12 with 10, 20 or 30 μM AMD3100. The FBS-free cells without 100 ng/ml CXCL12 or AMD3100 served as the control group. After the 7 day incubation, 20 μl MTT (5 mg/ml; Sigma, St. Louis, MO, USA) was added into each well and incubated for 4 h at 37°C. Culture medium was removed and 150 μl dimethylsulfoxide was added. The optical density (OD) was then measured using a model ELx800 microplate reader (Bio-Tech instruments inc.) at 490 nm. The cell viability was calculated using the equation: Cell viability (%) = (OD490nm of treatment/OD490nm of control) ×100%. |
| 浓度 | 30 μM |
| 处理时间 | 7 days |
| 动物实验 |
|---|
| 动物模型 | orthotopic animal model of OS in Ten 4-week-old female C3H mice |
| 配制 | PBS |
| 剂量 | 5 mg/kg every 2 days |
| 给药处理 | tail vein injection |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.2587 mL | 6.2935 mL | 12.587 mL |
| 5 mM | 0.2517 mL | 1.2587 mL | 2.5174 mL |
| 10 mM | 0.1259 mL | 0.6294 mL | 1.2587 mL |
