MK-571 sodium L-660711 sodium|cas:115103-85-0|西域试剂

MK-571 sodium L-660711 sodium,98.85%

产品编号：Bellancom-19989A| CAS NO：115103-85-0| 分子式：C₂₆H₂₆ClN₂NaO₃S₂| 分子量：537.07

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货号	价格	库存与货期
Bellancom-19989A	￥780.00	杭州北京（现货）
Bellancom-19989A	￥1300.00	杭州北京（现货）
Bellancom-19989A	￥2400.00	杭州北京（现货）
Bellancom-19989A	￥4200.00	杭州北京（现货）

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MK-571 sodium L-660711 sodium

产品介绍

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 K_i 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。

生物活性

MK-571 (L-660711) sodium is an orally active, potent and selective competitive leukotriene D₄ (LTD₄) receptor antagonist, with K_i 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.

体外研究

MK571 (15 μM, 1 h) sodium markedly suppresses constitutive and Ag-stimulated S1P secretion from RBL-2H3 cells and mast cells, and inhibits Fluo-3 efflux.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	RBL-2H3 cells, human LAD2 mast cells
Concentration:	15 μM
Incubation Time:	1 h
Result:	Inhibited S1P secretion by vector and SphK1 transfected RBL-2H3 cells, whereas it did not affect uptake and intracellular conversion of [3H]Sph to S1P. Inhibited Fluo-3 efflux, inhibited S1P export by LAD2 cells, and blocked Ag-stimulated release of S1P.

体内研究
(In Vivo)

MK-571 sodium (0-0.5 mg/kg, orally, once) produces dose-dependent inhibition of the duration of antigen-induced dyspnea in conscious sensitized rats treated with methysergide (3 μg/kg).
MK-571 sodium (0-1 mg/kg, orally, once) blocks LTD₄- and Ascaris-induced bronchoconstriction in conscious squirrel monkeys.
MK-571 sodium (0-25 mg/kg, Orally, daily, for 2 more weeks) shows reversal of hypoxic pulmonary hypertension (PH), and protects mice from hypoxic PH.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Hyperreactive rats (male and female, 200-400 g, pretreated intravenously with 3 μg/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 R_L and decreases in C_dyn 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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Hyperreactive rats (male and female, 200-400 g, pretreated intravenously with 3 μg/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 R_L and decreases in C_dyn 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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Hyperreactive rats (male and female, 200-400 g, pretreated intravenously with 3 μg/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 R_L and decreases in C_dyn 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.

性状

Solid

溶解性数据

In Vitro:

H₂O : 33.33 mg/mL (62.06 mM; Need ultrasonic)

DMSO : < 1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble or slightly soluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8620 mL	9.3098 mL	18.6195 mL
5 mM	0.3724 mL	1.8620 mL	3.7239 mL
10 mM	0.1862 mL	0.9310 mL	1.8620 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： PBS
Solubility: 33.33 mg/mL (62.06 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.17 mg/mL (4.04 mM); Clear solution

此方案可获得 ≥ 2.17 mg/mL (4.04 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.17 mg/mL (4.04 mM); Clear solution

此方案可获得 ≥ 2.17 mg/mL (4.04 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.87 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.87 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。