| 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].
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| 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) |
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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. |
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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. |
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| 分子量 |
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| 性状 |
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| Formula |
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| CAS 号 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 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)
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| 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
| 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 |
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请根据半岛bd体育手机客户端 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半岛bd体育手机客户端 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
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1.
请依序添加每种溶剂： PBS
Solubility: 33.33 mg/mL (62.06 mM); Clear solution; Need ultrasonic
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2.
请依序添加每种溶剂： 10% DMSO40%PEG3005%Tween-8045% 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。
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3.
请依序添加每种溶剂： 10% DMSO90% (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。
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4.
请依序添加每种溶剂： 10% DMSO90%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。
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以上所有助溶剂都可在本网站选购。
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