Valspodar

Valspodar 是一种 p-糖蛋白 (P-gp) 抑制剂，被广泛用作克服多药耐药性调节剂。

MCE (MedChemExpress) 是全球领先的科研化学品和生物活性化合物供应商，总部位于美国新泽西。MCE 的产品范围覆盖各种抑制剂、激动剂和化合物库。

Valspodar 是一种 p-糖蛋白 (P-gp) 抑制剂，被广泛用作克服多药耐药性调节剂。
Valspodar产品描述：Valspodar is a P-glycoprotein (P-gp) inhibitor widely used as overcoming multidrug resistance modulator.
In Vitro：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^[1]. Pretreatment with PSC833 decreases the IC₅₀ value of mitoxantrone in MDA-MB-435mdr cells to 0.4±0.02 μM in MDR cells and almost completely reverses the resistance of MDR cells to mitoxantrone^[3].
In Vivo：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 cyclosporine A^[2]. Preadministration of PSC833 to mice increases mitoxantrone fluorescent intensity in MDR tumor to 94% of that in the wild-type tumors^[3].


公司介绍：MedChemExpress(MCE)专注于各种抑制剂、激动剂、API及化合物库，总部位于美国新泽西，分别在瑞典和上海设有欧洲区子公司和区总代理，营销网点遍及20多个地区。MCE经过多年努力已成为生物活性小分子领域的供应商， 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域，PI3K、MAPK等近千个细分靶点，超过4000个活性小分子化合物现货，以及GPCR、API、离子通道等超过20种不同类型的化合物库，同时提供从毫克到千克的专业定制合成服务。
MCE 对每批产品都进行严格的LCMS和NMR检验，其产品已被近万名客户广泛使用并发表大量文章、；
MCE 定期增加各领域热门抑制剂、激动剂，不断扩增已有化合物库，以满足新的科研需求；
数千种产品在上海有充足备货，24-48小时内送达客户；
大量产品提供试用装； 已为多个知名企业、院校构建各种定制型化合物库。

Purity:98%
MWt:1214.6220
Formula:C63H111N11O12
SMILES:O=C([C@H](C(C)C)N(C)C([C@H](CC(C)C)N(C)C([C@H](CC(C)C)N(C)C([C@@H](C)NC([C@H](C)NC([C@H](CC(C)C)N(C)C([C@H](C(C)C)NC([C@H](CC(C)C)N(C)C(CN(C)C([C@H](C(C)C)N1)=O)=O)=O)=O)=O)=O)=O)=O)=O)N(C)[C@@H](C([C@H](C)C/C=C/C)=O)C1=O
Pathway:Membrane Transporter/Ion Channel;
Mechanisms:P-glycoprotein;
Research Area:Cancer




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