所有图片(3)
别名:
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 水合物, L-660711
经验公式（希尔记法）:
C26H26ClN2NaO3S2 · xH2O
CAS号:
分子量:
537.07 (anhydrous basis)
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
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质量水平
检测方案
≥95% (HPLC)
形式
powder
储存条件
desiccated
颜色
white to beige
溶解性
H2O: 15 mg/mL, clear
创始人
Merck & Co., Inc., Kenilworth, NJ, U.S.
运输
wet ice
储存温度
−20°C
SMILES字符串
O.[Na+].CN(C)C(=O)CCSC(SCCC([O-])=O)c1cccc(\C=C\c2ccc3ccc(Cl)cc3n2)c1
InChI
1S/C26H27ClN2O3S2.Na.H2O/c1-29(2)24(30)12-14-33-26(34-15-13-25(31)32)20-5-3-4-18(16-20)6-10-22-11-8-19-7-9-21(27)17-23(19)28-22;;/h3-11,16-17,26H,12-15H2,1-2H3,(H,31,32);;1H2/q;+1;/p-1/b10-6+;;
InChI key
MSHRPLRGSQECLY-DOLBFOAYSA-M
应用
MK-571钠盐水合物已被用于：
- 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
生化/生理作用
MK 571 是一种强效选择性白三烯 D4 (LTD4) 拮抗剂和 ABCC 多药耐药蛋白 1 (MRP1) 抑制剂。半胱氨酰白三烯 (CysLTs)，LTC4、LTD4 和 LTE4 通过两种不同的 G 蛋白偶联受体介导其作用。LTD4 是 CysLT1 受体的首选配体，而 LTC4 和 LTD4 与 CysLT2 受体的亲和力大致相等。MK 571 是一种选择性、口服活性 CysLT1 受体拮抗剂。阻断 LTD4 而非 LTC4 与人和豚鼠肺膜的结合，Ki 值分别为 0.22 nM 和 2.1 nM。MK 571 可有效阻断重组人和小鼠 CysLT1 受体的 LTD4 活化，但对阻断重组人或鼠 CysLT2 受体的 LTC4 或 LTD4 活化无效。它可能抑制 MRP1，并已显示克服获得性砷耐受性。
特点和优势
该化合物是由Merck & Co., Inc., Kenilworth, NJ, U.S.开发的。想要浏览其他由制药公司开发的化合物以及已批准药物/候选药物清单， 请单击此处。
警示用语：
Warning
危险声明
危险分类
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
靶器官
Respiratory system
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
dust mask type N95 (US), Eyeshields, Gloves
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