据报道，MK-571是[3H]白三烯D4（LTD4）与CysLT1受体结合的选择性竞争性抑制剂。LTD4已显示可诱导豚鼠气管和人肺膜收缩。半胱氨酰白三烯也被认为是重要的促炎介质，因此使MK-571成为抗发炎剂。该化合物表现出Mdr-1（多药抗性蛋白1）介导的转运的抑制特性。另外，研究表明该药剂可以增强细胞毒性剂对细胞的作用。MK-571是MRP1和CysLT1受体的抑制剂。 应用 MK-571钠盐已被用于： 作为外排抑制剂，监测多药耐药蛋白（MRP）的功能并避免其他转运蛋白的重复 在多种多形性胶质母细胞瘤（GBM）细胞系中，体外评估其对细胞增殖和二维迁移的影响 作为多药抗性（MDR）转运蛋白抑制剂，研究其在卵巢癌细胞中的作用 作为ABCC1/2的特异性抑制剂，用于转运、毒性、流式细胞术和砷外排的研究 MK-571 has been reported to be a selective competitive inhibitor of [3H]leukrotriene D4 (LTD4) binding to CysLT1 receptors. LTD4 has been shown to induce contractions in guinea pig trachea and human lung membranes. Cysteinyl leukotrienes have also been identified as important pro-inflammatory mediators, therefore making MK-571 an anti-inflammatory agent. This compound demonstrates inhibitory characteristics of Mdr-1 (multidrug resistance protein-1) mediated transport. Additionally, studies suggest that this agent can augment the effects of cytotoxic agents on cells|in vitro|. MK-571 is an inhibitor of MRP1 and CysLT1 Receptor.
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MK-571 sodium
CAS number：115103-85-0 molecular formula：C26H26ClN2O3S2·Na
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| Chinese alias | 5-(3-(2-(7-氯喹啉-2-基)乙烯基)苯基)-8-二甲基氨基甲酰-4,6-二硫杂辛酸 钠盐 | ||
| English alias | MK-571 (sodium salt) | 1263184-04-8 | sodium;3-[[3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-[3-(dimethylamino)-3-oxopropyl]sulfanylmethyl]sulfanylpropanoate | 1,4-piperazinediethanesulfonic acid monosodium salt | J-003253 | Tox21_112060 | NCGC0016350 | ||
| CAS number | 115103-85-0 | molecular formula | C26H26ClN2O3S2·Na |
| molecular weight | 537.07 g/mol | Exact mass | ≥96% |
| PSA | 124.000 Ų | logp | - |
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