MK-571 (Synonyms: L-660711)

目录号: HY-19989 纯度: 98.66%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

MK-571 (L-660711) 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 也是一种 MRP4 和 ABCC1 (MRP1) 抑制剂。MK-571 可抑制构成性和抗原刺激的 S1P 释放。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

MK-571 Chemical Structure

CAS No. : 115104-28-4

1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
1 mg	￥344	In-stock
5 mg	￥780	In-stock
10 mg	￥1244	In-stock
25 mg	￥2400	In-stock
50 mg	￥4200	In-stock
100 mg	￥5880	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of MK-571:

MK-571 sodium In-stock

MCE 顾客使用本产品发表的 24 篇科研文献

MK-571 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Leukotriene Receptor 亚型特异性产品:

查看所有亚型

LTB₄ LTC₄/CysLT₂ LTD₄/CysLT₁ LTE₄

查看 LPL Receptor 亚型特异性产品:

查看所有亚型

LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

生物活性
纯度 & 产品资料
参考文献

生物活性

MK-571 (L-660711) 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 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release^[1]^[2]^[3].

IC₅₀ & Target^[1]

LTD₄

0.22 nM (Ki, In guinea pig lung)

LTD₄

2.1 nM (Ki, In human lung)

LTD₄

10.5 (pA2, on guinea pig ileum)

LTE₄

10.4 (pA2, on guinea pig ileum)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.06 μM Compound: MK571	Potentiation of etoposide-induced cytotoxicity against HEK293 cells assessed as etoposide IC50 at 25000 nM after 72 hrs by CCK8 assay (Rvb = 0.11 +/- 0.03 nM) Potentiation of etoposide-induced cytotoxicity against HEK293 cells assessed as etoposide IC50 at 25000 nM after 72 hrs by CCK8 assay (Rvb = 0.11 +/- 0.03 nM)	[PMID: 27504669]
HEK293	IC₅₀	0.16 nM Compound: MK-571	Effect on etoposide-induced cytotoxicity against HEK293 cells by measuring etoposide IC50 at 25 uM after 72 hrs by CCK8 assay (Rvb =0.21 +/- 0.04 uM) Effect on etoposide-induced cytotoxicity against HEK293 cells by measuring etoposide IC50 at 25 uM after 72 hrs by CCK8 assay (Rvb =0.21 +/- 0.04 uM)	[PMID: 32347726]
HEK293	IC₅₀	2.9 μM Compound: MK-571	Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting	[PMID: 22541068]
HEK293	IC₅₀	4.4 μM Compound: MK-571	Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting	[PMID: 22541068]
HEK293	IC₅₀	5.22 μM Compound: MK571	Inhibition of human ABCC1 transfected in HEK293 cells assessed as potentiation of etoposide-induced cytotoxicity by measuring etoposide IC50 at 25000 nM after 72 hrs by CCK8 assay (Rvb = 38.54 +/- 5.62 nM) Inhibition of human ABCC1 transfected in HEK293 cells assessed as potentiation of etoposide-induced cytotoxicity by measuring etoposide IC50 at 25000 nM after 72 hrs by CCK8 assay (Rvb = 38.54 +/- 5.62 nM)	[PMID: 27504669]
HEK293	IC₅₀	6.4 μM Compound: MK-571	Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting	[PMID: 22541068]
L929	IC₅₀	> 100 μM Compound: MK571	Cytotoxicity against mouse L929 cells assessed as reduction in cell survival after 5 days by MTS assay Cytotoxicity against mouse L929 cells assessed as reduction in cell survival after 5 days by MTS assay	[PMID: 30351934]
MDCK	IC₅₀	> 1000 nM Compound: MK-571	Inhibition of ABCC2 overexpressed in MDCK cells at 100 uM by flow cytometric-based chloromethylfluorescein-diacetate accumulation assay Inhibition of ABCC2 overexpressed in MDCK cells at 100 uM by flow cytometric-based chloromethylfluorescein-diacetate accumulation assay	[PMID: 19170519]
MDCK	EC₅₀	2.85 μM Compound: MK-571	Inhibition of MRP1 expressed in MDCK cells assessed as calcein AM accumulation by fluorescence assay Inhibition of MRP1 expressed in MDCK cells assessed as calcein AM accumulation by fluorescence assay	[PMID: 20684594]
NCI-H69	EC₅₀	12.4 μM Compound: MK-571	Modulation of MRP1 mediated drug efflux in doxorubicin-resistant human H69 cells assessed as accumulation of calcein AM incubated for 15 mins prior to calcein AM addition measured after 30 mins by fluorescence analysis Modulation of MRP1 mediated drug efflux in doxorubicin-resistant human H69 cells assessed as accumulation of calcein AM incubated for 15 mins prior to calcein AM addition measured after 30 mins by fluorescence analysis	[PMID: 25311564]

体外研究
(In Vitro)

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^[3]。

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

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（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^[1]。
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^[1]。
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^[2]。

MCE 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)^[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 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^[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 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)^[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

515.09

Formula

C₂₆H₂₇ClN₂O₃S₂

CAS 号

115104-28-4

性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 125 mg/mL (242.68 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9414 mL	9.7070 mL	19.4141 mL
5 mM	0.3883 mL	1.9414 mL	3.8828 mL
10 mM	0.1941 mL	0.9707 mL	1.9414 mL

查看完整储备液配制表

* 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 (protect from light)。-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。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 98.66%

选择批次：

Data Sheet (625 KB) SDS (393 KB)

COA (285 KB) HNMR (281 KB) LCMS (88 KB)

产品使用指南 (1538 KB)

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. [Content Brief]

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

[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. [Content Brief]

MK-571 相关分类

Inflammation/Immunology

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9414 mL	9.7070 mL	19.4141 mL	48.5352 mL
	5 mM	0.3883 mL	1.9414 mL	3.8828 mL	9.7070 mL
	10 mM	0.1941 mL	0.9707 mL	1.9414 mL	4.8535 mL
	15 mM	0.1294 mL	0.6471 mL	1.2943 mL	3.2357 mL
	20 mM	0.0971 mL	0.4854 mL	0.9707 mL	2.4268 mL
	25 mM	0.0777 mL	0.3883 mL	0.7766 mL	1.9414 mL
	30 mM	0.0647 mL	0.3236 mL	0.6471 mL	1.6178 mL
	40 mM	0.0485 mL	0.2427 mL	0.4854 mL	1.2134 mL
	50 mM	0.0388 mL	0.1941 mL	0.3883 mL	0.9707 mL
	60 mM	0.0324 mL	0.1618 mL	0.3236 mL	0.8089 mL
	80 mM	0.0243 mL	0.1213 mL	0.2427 mL	0.6067 mL
	100 mM	0.0194 mL	0.0971 mL	0.1941 mL	0.4854 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

您最近查看的产品:

产品名称：

* 需求量：

* 客户姓名：

* Email：

* 电话：

* 公司或机构名称：

留言给我们：

MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。	站点地图隐私声明
沪ICP备15051369号-4 上海工商沪公网安备31011502019417 沪(浦)应急管危经许[2021]201709(QFYS) 营业执照（三证合一）
Copyright © 2013-2025 MedChemExpress. All Rights Reserved.

MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

MK-571 (Synonyms: L-660711)

Customer Review

Other Forms of MK-571:

MCE 顾客使用本产品发表的 24 篇科研文献