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MK-571 sodium
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
MK-571 sodium图片
CAS NO:115103-85-0
包装与价格：
包装价格(元)
10 mM * 1 mL in Water电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品名称
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。
生物活性

MK-571 (L-660711) sodium is an orally active, potent and selective competitiveleukotriene D4(LTD4) receptorantagonist, withKivalues 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 proteinMRP4 (ABCC4)andABCC1 (MRP1). MK-571 sodium inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release[1][2][3].

IC50& Target[1]

LTD4

0.22±0.15 nM (Ki, In guinea pig lung)

LTD4

2.1±1.8 nM (Ki, In human lung)

LTD4

10.5 (pA2)

LTE4

10.4 (pA2)

体外研究
(In Vitro)

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[3].

Cell Viability Assay[3]

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)[1].
MK-571 sodium (0-1 mg/kg, orally, once) blocks LTD4- and Ascaris-induced bronchoconstriction in conscious squirrel monkeys[1].
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[2].

Animal Model:Hyperreactive rats (male and female, 200-400 g, pretreated intravenously with 3 μg/kg methysergide, 5 min before antigen chdlenge)[1]
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 ED50values 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 ED50of 0.068 (95% CI, 0.83-0.14) mg/kg.
Animal Model:Csnscisus squirrel msnkeys[1]
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 RLand decreases in Cdynat 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)[2]
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.
分子量

537.07

性状

Solid

Formula

C26H26ClN2NaO3S2

CAS 号

115103-85-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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℃)(insoluble or slightly soluble)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.8620 mL9.3098 mL18.6195 mL
5 mM0.3724 mL1.8620 mL3.7239 mL
10 mM0.1862 mL0.9310 mL1.8620 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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-CDin 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 μL20% 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。

*以上所有助溶剂都可在本网站选购。