中文名 | MK-571 (sodium salt) |
英文名 | MK-571 (sodium salt) |
别名 | MK-571钠 化合物PROPANOIC ACID (E)-3-[[[3-[2-(7-氯-2-喹啉基)乙烯基]苯基][[3-(二甲基氨基)-3-氧代丙基]硫基]甲基]硫基]丙酸钠盐 |
英文别名 | 711 L-660 MK571 MK 571 L660711 L-660711 MK-571 Sodium Verlukast sodium MK571 SODIUM SALT MK 571 SODIUM SALT MK-571 SODIUM SALT L660711 SODIUM SALT L-660711 SODIUM SALT MK-571 (sodium salt) L 660711 SODIUM SALT MK-571 SODIUM HYDRATE MK-571 sodium salt hydrate 5-(3-(2-(7-Chloroquinolin-2-yl)ethenyl)phenyl)-8-dimethylcarbamyl-4,6-dithiaoctanoic acid sodium salt hydrate (E)-3-[[[3-[2-(7-Chloro-2-quinolinyl)ethenyl]phenyl][[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]propanoic acid sodium salt Propanoic acid, 3-[[[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl][[3-(diMethylaMino)-3-oxopropyl]thio]Methyl]thio]-, sodiuM salt, (E)- |
CAS | 115103-85-0 |
化学式 | C26H26ClN2NaO3S2 |
分子量 | 537.06901 |
溶解度 | H2O: 可溶15mg/mL,澄清 |
存储条件 | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
外观 | 粉末 |
颜色 | white to beige |
体外研究 | MK-571 (L660,711) is a potent and selective competitive inhibitor of [ 3 H]leukotriene D4 binding in guinea pig (K i value, 0.22 nM) and human (K i value, 2.1 nM) lung membranes. MK-571 is essentially inactive versus [ 3 H]LTC4 binding with IC 50 values of 23±11 μM (n=16) and 32 μM (n=1) in guinea pig and human lung, respectively. MK-571 competitively antagonizes contractions of guinea pig trachea and ileum induced by leukotriene (LT) D 4 (respective pA 2 values, 9.4 and 10.5) and LTE4 (respective pA 2 values, 9.1 and 10.4) and contractions of human trachea induced by LTD 4 (pA 2 value, 8.5). MK-571 (58 nM) antagonizes contractions of guinea pig trachea induced by LTC 4 in the absence (dose ratio=28) but not in the presence of 45 mM L-serine borate (dose ratio less than 2). MK-571 (19μM) does not block contractions of guinea pig trachea induced by histamine, acetylcholine, 5-hydroxytryptamine, PGF 2 alpha, U-44069, or PGD 2 . In the presence of atropine, mepyramine, and indomethacin, MK-571 (19 μM) inhibits a small component of the response to antigen on guinea pig trachea but completely blocked anti-IgE-induced contractions of human trachea. |
体内研究 | MK-571 (L-660,711; i.v.) antagonizes bronchoconstriction induced in anesthetized guinea pigs by i.v. LTC 4 , LTD 4 , and LTE 4 but does not block bronchoconstriction to arachidonic acid, U-44069, 5-hydroxytryptamine, histamine, or acetylcholine. Intraduodenal MK-571 antagonizes LTD 4 (0.2-12.8 μg/kg)-induced bronchoconstriction in guinea pigs, and p.o. MK-571 blockes LTD 4 - and Ascaris-induced bronchoconstriction in conscious squirrel monkeys and ovalbumin-induced bronchoconstriction in conscious sensitized rats treated with methysergide (3 μg/kg). Hypoxia-exposed WT mice are treated with either saline or MK-571 (5 mg/kg/d or 25 mg/kg/d) for 2 more weeks while being maintain in hypoxic conditions. Saline-treated mice display all the hallmarks of PH (i.e., an increase in RVSP, Fulton index, and arterial wall thickness). However, following hypoxia, MK-571-treated mice display lower RVSP and Fulton index and a decrease in the medial thickening of small pulmonary arteries and arterioles. |
危险品标志 | Xi - 刺激性物品 |
风险术语 | 36/37/38 - 刺激眼睛、呼吸系统和皮肤。 |
安全术语 | S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S36/37 - 穿戴适当的防护服和手套。 |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.862 ml | 9.31 ml | 18.62 ml |
5 mM | 0.372 ml | 1.862 ml | 3.724 ml |
10 mM | 0.186 ml | 0.931 ml | 1.862 ml |
5 mM | 0.037 ml | 0.186 ml | 0.372 ml |
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