MK-571 (L-660711) sodium 是一种口服有效、选择性的和竞争性的白三烯 D4 (LTD4) 受体拮抗剂，在豚鼠和人肺膜中的 Ki 值分别为 0.22 和 2.1 nM。MK-571 sodium 也是一种多药耐药相关蛋白 MRP4 (ABCC4) 和 ABCC1 (MRP1) 抑制剂。MK-571 sodium 可抑制构成性和抗原刺激的 S1P 释放。
| CAS No. | 115103-85-0 |
| 生物活性 | MK-571 (L-660711) sodium is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 sodium is also a inhibitor of multidrug resistance-associated protein MRP4 (ABCC4) and ABCC1 (MRP1). MK-571 sodium inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release. |
| 分子式 | C26H26N2O3S2Cl-.Na+ |
| 分子量 | 537.07 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder -20°C 3 years |
| 溶解性数据 | DMSO : ≥ 33 mg/mL (61.44 mM) H2O : 12.5 mg/mL (23.27 mM; Need ultrasonic) |
| 体内研究 | MK-571 (L-660,711; i.v.) antagonizes bronchoconstriction induced in anesthetized guinea pigs by i.v. LTC4, LTD4, and LTE4 but does not block bronchoconstriction to arachidonic acid, U-44069, 5-hydroxytryptamine, histamine, or acetylcholine. Intraduodenal MK-571 antagonizes LTD4 (0.2-12.8 μg/kg)-induced bronchoconstriction in guinea pigs, and p.o. MK-571 blockes LTD4- 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. |
| 体外研究 | MK-571 (L660,711) is a potent and selective competitive inhibitor of [H]leukotriene D4 binding in guinea pig (Ki value, 0.22 nM) and human (Ki value, 2.1 nM) lung membranes. MK-571 is essentially inactive versus [H]LTC4 binding with IC50 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) D4 (respective pA2 values, 9.4 and 10.5) and LTE4 (respective pA2 values, 9.1 and 10.4) and contractions of human trachea induced by LTD4 (pA2 value, 8.5). MK-571 (58 nM) antagonizes contractions of guinea pig trachea induced by LTC4 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, PGF2 alpha, U-44069, or PGD2. 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. |
| 文献 | •Biomed Pharmacother. 2020 Sep;129:110506. •Biomed Pharmacother. 2018 Oct;106:1563-1569. •Int J Nanomedicine. 2019 Nov 27;14:9217-9234. •Arch Toxicol. 2020 Nov;94(11):3799-3817. •Viruses. 2019 Apr 24;11(4):378. •Toxicol Lett. 2020 Jul 1;327:9-18. •J Pharmaceut Biomed. 2020 Sep 10;189:113441. •Regul Toxicol Phar. 2019 Nov;108:104449. •Xenobiotica. 2020 Mar;50(3):354-362. •Pharmazie. 2020 Jan 2;75(1):18-22. |
| 纯度及产品资料 | ≥98% |
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