生物活性
Biricodar (VX-710, Incel)是一种能够同时抑制P-gp和MRP活性的逆转剂，逆转活性很高，约为第一代抑制剂的100倍以上。
化学数据
| 分子量 | 603.7 |
| 分子式 | C34H41N3O7 |
| CAS号 | 174254-13-8 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO |
| 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 | HL60 cells line |
| 方法 | Cytotoxicity Assays.
To study cytotoxicity in suspension cell lines, cells were plated in 96-well tissue culture plates at a density of 10,000 cells/well in RPMI 1640 supplemented with 10% FCS, 2 mm l-glutamine, 20 units/ml penicillin, and 20 μg/ml streptomycin. Drug was added to the culture medium to achieve final concentrations of 0.3 nm to 10 μm, with half-log increments, with and without VX-710 at a final concentration of 2.5 μM. The final volume of medium per well was 100 μl. Cells were incubated for 96 h at 37°C in a fully humidified atmosphere of 5% CO2 in air. Cell growth was assessed by the WST-1 colorimetric assay (Roche Diagnostics GmbH, Mannheim, Germany; Ref. 29 ), performed according to the manufacturer’s instructions. Briefly, 10 μl of WST-1 were added to each well, and culture plates were returned to the incubator for an additional 4 h. Subsequently, the absorbance at 450 nm (A450) and 600 nm (A600, background) was read for each well using a Microtek multiwell plate reader. Each drug exposure condition was assessed in quadruplicate. |
| 浓度 | 2.5 μM |
| 处理时间 | 96 h |
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 | 1.6565 mL | 8.2823 mL | 16.5645 mL |
| 5 mM | 0.3313 mL | 1.6565 mL | 3.3129 mL |
| 10 mM | 0.1656 mL | 0.8282 mL | 1.6565 mL |
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