产品
编 号：F046686
分子式：C26H26ClN2NaO3S2
分子量：537.07
分子式：C26H26ClN2NaO3S2
分子量：537.07
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 115103-85-0
产品详情
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.
体内研究：
MK-571 sodium (0-0.5 mg/kg，口服，单剂量) 在用 Methysergide (3 μg/kg) 处理的有意识的致敏大鼠中对抗原诱导的呼吸困难持续时间产生剂量依赖性抑制。 MK-571 sodium (0-1 mg/kg, 口服，1 次) 有意识的松鼠猴中阻断 LTD4 和 Ascaris 诱导的支气管收缩。 MK-571 sodium (0-25 mg/kg，口服，每日，持续 2 周以上) 显示出缺氧性肺动脉高压 (PH) 的逆转，并保护小鼠缺氧 PH。Animal Model:Hyperreactive rats (male and female, 200-400 g, pretreated intravenously with 3μg/kg methysergide, 5 min before antigen chdlenge)
Dosage:0.5, 0.15, and 0.05 mg/kg
Administration:Orally, once, 1 or 4 h before challenge
Result:Produced dose-dependent inhibition of the duration of antigen-induced dyspnea, with ED50 values of 0.13 (95% confidence interval (CI), 0.03-0.62) and 0.11 (95% CI, 0.009-1.47) mg/kg, respectively. MK-571 was even more active when administered orally as a suspension in 1% Methocel (4 h pretreatment), with an ED50 of 0.068 (95% CI, 0.83-0.14) mg/kg.
Animal Model:Csnscisus squirrel msnkeys
Dosage:0.1, 0.5, and 1 mg/kg
Administration:Orally, once, 2 h prior to challenge with Ascaris antigen
Result:Produced significant inhibition of the bronchoconstriction at 0.5 mg/kg, produced significant inhibition of the increases in RL and decreases in Cdyn at 1 mg/kg.
Animal Model:FVB (Friend virus B-type) mice (Mrp4–/– and WT, 6 weeks old, exposed to chronic hypoxia (10% O2) in a ventilated chamber for 28 days)
Dosage:0, 5, and 25 mg/kg
Administration:Orally, daily, for 2 more weeks, maintain in hypoxic conditions
Result:Showed reversal of hypoxic pulmonary hypertension (PH), and mice were protected from hypoxic PH. MK-571-treated mice displayed lower RVSP and Fulton index and a decrease in the medial thickening of small pulmonary arteries and arterioles.
体外研究：
MK571 sodium (15 μM，1 小时) 显著抑制 RBL-2H3 细胞和肥大细胞的组成型和 Ag 刺激的 S1P 分泌，并抑制 Fluo-3 流出。
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.
体内研究：
MK-571 sodium (0-0.5 mg/kg，口服，单剂量) 在用 Methysergide (3 μg/kg) 处理的有意识的致敏大鼠中对抗原诱导的呼吸困难持续时间产生剂量依赖性抑制。 MK-571 sodium (0-1 mg/kg, 口服，1 次) 有意识的松鼠猴中阻断 LTD4 和 Ascaris 诱导的支气管收缩。 MK-571 sodium (0-25 mg/kg，口服，每日，持续 2 周以上) 显示出缺氧性肺动脉高压 (PH) 的逆转，并保护小鼠缺氧 PH。Animal Model:Hyperreactive rats (male and female, 200-400 g, pretreated intravenously with 3μg/kg methysergide, 5 min before antigen chdlenge)
Dosage:0.5, 0.15, and 0.05 mg/kg
Administration:Orally, once, 1 or 4 h before challenge
Result:Produced dose-dependent inhibition of the duration of antigen-induced dyspnea, with ED50 values of 0.13 (95% confidence interval (CI), 0.03-0.62) and 0.11 (95% CI, 0.009-1.47) mg/kg, respectively. MK-571 was even more active when administered orally as a suspension in 1% Methocel (4 h pretreatment), with an ED50 of 0.068 (95% CI, 0.83-0.14) mg/kg.
Animal Model:Csnscisus squirrel msnkeys
Dosage:0.1, 0.5, and 1 mg/kg
Administration:Orally, once, 2 h prior to challenge with Ascaris antigen
Result:Produced significant inhibition of the bronchoconstriction at 0.5 mg/kg, produced significant inhibition of the increases in RL and decreases in Cdyn at 1 mg/kg.
Animal Model:FVB (Friend virus B-type) mice (Mrp4–/– and WT, 6 weeks old, exposed to chronic hypoxia (10% O2) in a ventilated chamber for 28 days)
Dosage:0, 5, and 25 mg/kg
Administration:Orally, daily, for 2 more weeks, maintain in hypoxic conditions
Result:Showed reversal of hypoxic pulmonary hypertension (PH), and mice were protected from hypoxic PH. MK-571-treated mice displayed lower RVSP and Fulton index and a decrease in the medial thickening of small pulmonary arteries and arterioles.
体外研究：
MK571 sodium (15 μM，1 小时) 显著抑制 RBL-2H3 细胞和肥大细胞的组成型和 Ag 刺激的 S1P 分泌，并抑制 Fluo-3 流出。
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