伐司扑达

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产品编号 D50701
英文名称 Valspodar
中文名称 伐司扑达
别    名 PSC 833; P-glycoprotein inhibitor; 3′-Keto-bmt(1)-Val(2)-cyclosporin a; Cyclosporin A, 6-((R-(E))-6,7-didehydro-N,4-dimethyl-3-oxo-L-2-aminooctanoic acid)-7-L-valine-;   戊司泊达; P-糖蛋白抑制剂; P糖蛋白抑制剂;
保存条件 Store at -20℃ for 3 year(Powder); In DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.
注意事项 This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications.
产品介绍 基本信息:
CAS:121584-18-7
分子式:C36H70N4O5
分子量:1214.62
纯度:99%
溶解性:DMSO (12 mg/mL, 9.88 mM;)
性状:白色到米色粉末

产品简介:
伐司朴达(Valspodar; PSC 833)是一种选择性的 P-糖蛋白抑制剂,已被用作化学增敏剂用于实验性癌症的研究。
作用靶点:P-glycoprotein;  
作用通路:Membrane Transporter/Ion Channel; 
体外研究:Cancer

体外研究:Valspodar (PSC833) has no cytotoxicity effects at up to the concentration of 0.75μg/mL. Valspodar (0.25, 0.5 and 0.75μg/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 0.75μg/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 IC50 value of NSC 279836 in MDA-MB-435mdr cells to 0.4±0.02μM in MDR cells and almost completely reverses the resistance of MDR cells to NSC 279836.

体内研究:valspodar (10mg/kg,o.p.) exhibits minimal blood-cell partitioning as reflected in its low mean blood-to-plasma ratio of approximately 0.52. Valspodar isplays properties of slow learance and a large volume of distribution. Valspodar shows properties of low hepatic extraction and ide 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.