中文同义词:
伐司扑达;戊司泊达;P-糖蛋白抑制剂(VALSPODAR);伐司朴达
英文同义词:
Valspodar;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-;Psc 833;Sdz psc 833;Sdz-psc-833;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];6-[(2S,4R,6E)-4-methyl-2-(methylamino)-3-oxo-6-octenoicacid]-7-L-valine-cyclosporinA
相关类别:
抑制剂;细胞生物学试剂;Intermediates Fine Chemicals;Peptides;Pharmaceuticals
比旋光度
D20 -255.1° (c = 0.5 in CHCl3)
沸点
1290.1±65.0 °C(Predicted)
密度
1.015±0.06 g/cm3(Predicted)
酸度系数(pKa)
12.45±0.70(Predicted)
生物活性
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。
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.
