MK-571 sodium salt hydrate|115103-85-0|(L-660711 sodium)-陌孚医药/Medlife

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MK-571 sodium salt hydrate (Synonyms: L-660711 sodium)

目录号: PC11421 纯度: ≥98%

CAS No. :115103-85-0

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中文名称	MK-571 sodium salt hydrate
中文别名	(E)-3-[[[3-[2-(7-氯-2-喹啉基)乙烯基]苯基][[3-(二甲基氨基)-3-氧代丙基]硫基]甲基]硫基]丙酸钠盐;MK-571 (sodium salt)
英文名称	MK-571 sodium salt hydrate
英文别名	Sodium (E)-3-(((3-(2-(7-chloroquinolin-2-yl)vinyl)phenyl)((3-(dimethylamino)-3-oxopropyl)thio)methyl)thio)propanoate; MK-571 sodium salt hydrate;L-660711 sodium salt;MK 571 (sodium salt);MK-571 SODIUM HYDRATE;L660711 sodium salt;MK571 sodium salt;5-(3-(2-(7-Chloroquinolin-2-yl)ethenyl)phenyl)-8-dimethylcarbamyl-4,6-dithiaoctanoic acid sodium salt hydrate;(E)-3-[[[3-[2-(7-Chloro-2-quinolinyl)ethenyl]phenyl][[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]propanoic acid sodium salt;Propanoic acid, 3-[[[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl][[3-(diMethylaMino)-3-oxopropyl]thio]Methyl]thio]-, sodiuM salt, (E)-;MK-571 (sodium salt);MK-571 sodium salt
Cas No.	115103-85-0
分子式	C₂₆H₂₆N₂O₃S₂Cl-^.Na+
分子量	537.07
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.

性状

Solid

IC50 & Target[1][2]

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.

Medlife 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.

Medlife 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.

运输条件

Room temperature or refrigerated transportation.

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)

参考文献

[1]. Jones TR, et al. Pharmacology of L-660,711 (MK-571): a novel potent and selective leukotriene D₄ receptor antagonist. Can J Physiol Pharmacol. 1989 Jan;67(1):17-28. [Information]

[2]. Hara Y, et al. Inhibition of MRP4 prevents and reverses pulmonary hypertension in mice. J Clin Invest. 2011 Jul;121(7):2888-97. [Information]

[3]. Mitra P, et al. Role of ABCC1 in export of sphingosine-1-phosphate from mast cells. Proc Natl Acad Sci U S A. 2006 Oct 31;103(44):16394-9. [Information]

溶解度数据

体外研究:

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

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

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： PBS
Solubility: 33.33 mg/mL (62.06 mM); Clear solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 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 ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 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.

建议依照次序添加每种溶剂： 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。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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