MK-571 sodium salt hydrate

MK571 sodium salt是特异性CysLT1（半胱氨酰-白三烯1型受体）拮抗剂[1]。

半胱氨酰白三烯受体1简称为CYSLTR1，是半胱氨酰白三烯（LT）的受体，在人体内介导多种过敏和超敏反应[2]。

体外实验：MK571是多药耐药蛋白-2（ABCC2，Mrp2）抑制剂，被广泛用于证明Mrp2在药物、异生素及其共轭物的细胞外排中的作用。顶端施用MK571显著减少来自Caco-2/TC7单层的黄酮醇缀合物的顶端和基底外侧流出。MK571抑制K-4'-O-GlcA合成的估算的Ki为19.7 μM。MK571以剂量依赖性方式抑制Caco-2细胞所有黄酮醇葡糖苷酸和硫酸盐的细胞内生物合成。MK571显著抑制Caco-2的无细胞提取物中kaempferol的2相共轭，并竞争性抑制kaempferol-4′-O-glucuronide的生成。这些数据表明MK571除了抑制MRP2之外，还是肠上皮细胞2相共轭的潜在抑制剂[3]。

参考文献：
[1] Thivierge M, Turcotte S, Rola-Pleszczynski M, et al.  Enhanced cysteinyl-leukotriene type 1 receptor expression in T cells from house dust mite-allergic individuals following stimulation with Der p[J]. Journal of immunology research, 2015, 2015.
[2] Singh RK, Tandon R, Dastidar SG, Ray A (November 2013).  "A review on leukotrienes and their receptors with reference to asthma".The Journal of Asthma.50(9): 922–31.
[3] Barrington R D, Needs P W, Williamson G, et al.  MK571 inhibits phase-2 conjugation of flavonols by Caco-2/TC7 cells, but does not specifically inhibit their apical efflux[J]. Biochemical pharmacology, 2015, 95(3): 193-200.