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编 号：F046689
分子式：C26H27ClN2O3S2
分子量：515.09
分子式：C26H27ClN2O3S2
分子量：515.09
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CAS No: 115104-28-4
产品详情
生物活性：
MK-571 (L-660711) 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 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release.
体内研究：
MK-571（0-0.5 mg/kg，口服，一次）对接受美西麦角 (3 μg/kg) 治疗的清醒致敏大鼠中抗原诱导的呼吸困难持续时间产生剂量依赖性抑制。MK-571（0-1 mg/kg，口服，一次）可阻断有意识的松鼠猴中 LTD4- 和蛔虫诱导的支气管收缩。MK-571（0-25 mg/kg，口服，每天，持续 2 周以上）可逆转缺氧性肺动脉高压 (PH)，并保护小鼠免受缺氧性 PH 的影响。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（15 μM，1 小时）显着抑制 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 外排。
MK-571 (L-660711) 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 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release.
体内研究：
MK-571（0-0.5 mg/kg，口服，一次）对接受美西麦角 (3 μg/kg) 治疗的清醒致敏大鼠中抗原诱导的呼吸困难持续时间产生剂量依赖性抑制。MK-571（0-1 mg/kg，口服，一次）可阻断有意识的松鼠猴中 LTD4- 和蛔虫诱导的支气管收缩。MK-571（0-25 mg/kg，口服，每天，持续 2 周以上）可逆转缺氧性肺动脉高压 (PH)，并保护小鼠免受缺氧性 PH 的影响。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（15 μM，1 小时）显着抑制 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 外排。
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