| CAS NO: | 115103-85-0 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 537.07 (anhydrous basis) |
| Cas No. | 115103-85-0 |
| Formula | C26H26ClN2NaO3S2·xH2O |
| Synonyms | L-660711 |
| Solubility | ≥10.3 mg/mL in DMSO with gentle warming and ultrasonic; ≥122.2 mg/mL in H2O; ≥8.3 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 5-(3-(2-(7-Chloroquinolin-2-yl)ethenyl)phenyl)-8-dimethylcarbamyl-4,6-dithiaoctanoic acid sodium salt hydrate |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
m.cnreagent.com