戊司泊达
Valspodar(Valspodar)
CAS: 121584-18-7
化学式: C63H111N11O12
| 中文名 | Valspodar |
| 英文名 | Valspodar |
| 别名 | 伐司扑达 伐司朴达 戊司泊达 P-糖蛋白抑制剂(VALSPODAR) |
| 英文别名 | Psc 833 Valspodar Sdz psc 833 Sdz-psc-833 3'-Keto-bmt(1)-Val(2)-cyclosporin a 6-[(2S,4R,6E)-4-methyl-2-(methylamino)-3-oxo-6-octenoicacid]-7-L-valine-cyclosporinA Cyclosporin A, 6-((R-(E))-6,7-didehydro-N,4-dimethyl-3-oxo-L-2-aminooctanoic acid)-7-L-valine- Cyclo[[(2S,4R,6E)-4-methyl-2-(methylamino)-3-oxo-6-octenoyl]-L-valyl-N-methylglycyl-N-methyl-L-leucyl-L-valyl-N-methyl-L-leucyl-L-alanyl-D-alanyl-N-methyl-L-leucyl-N-methyl-L-leucyl-N-methyl-L-valyl] |
| CAS | 121584-18-7 |
| EINECS | 1312995-182-4 |
| 化学式 | C63H111N11O12 |
| 分子量 | 1214.62 |
| 密度 | 1.015±0.06 g/cm3(Predicted) |
| 熔点 | 143-145°C |
| 沸点 | 1290.1±65.0 °C(Predicted) |
| 比旋光度 | D20 -255.1° (c = 0.5 in CHCl3) |
| 溶解度 | 氯仿 (微溶) 、甲醇 (微溶) |
| 酸度系数 | 12.45±0.70(Predicted) |
| 存储条件 | -20°C |
| 外观 | 粉末 |
| 颜色 | white to beige |
| 体外研究 | Valspodar (PSC 833) has no cytotoxicity effects at up to the concentration of 0.75 μg/mL. Valspodar (0.25, 0.5 and 0.75 μg/mL) and DOX-L are added to the DOX resistant cells, and cell kill efficacy of MDR cell type increases significantly when valspodar is administered alongside DOX-L. Valspodar (0.5 and 0.75 μg/mL), in combination with all concentrations of DOX, are most toxic and kill more than 70% of the resistant cells. Pretreatment with PSC833 decreases the IC 50 value of NSC 279836 in MDA-MB-435mdr cells to 0.4±0.02 μM in MDR cells and almost completely reverses the resistance of MDR cells to NSC 279836. |
| 体内研究 | valspodar (10 mg/kg, o.p.) exhibits minimal blood-cell partitioning as reflected in its low mean blood-to-plasma ratio of approximately 0.52. Valspodar displays properties of slow clearance and a large volume of distribution. Valspodar shows properties of low hepatic extraction and wide distribution, similar to that of its structural analogue CsA. Preadministration of PSC833 to mice increases NSC 279836 fluorescent intensity in MDR tumor to 94% of that in the wild-type tumors. |
| WGK Germany | 3 |
戊司泊达 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 0.823 ml | 4.117 ml | 8.233 ml |
| 5 mM | 0.165 ml | 0.823 ml | 1.647 ml |
| 10 mM | 0.082 ml | 0.412 ml | 0.823 ml |
| 5 mM | 0.016 ml | 0.082 ml | 0.165 ml |
最后更新：2024-01-02 23:10:35
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