MK-571 (Synonyms: L-660711)

Name: MK-571
Brand: MedChemExpress
SKU: HY-19989
Rating: 5.0 (24 reviews)

Cat. No.: HY-19989 Purity: 98.66%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

MK-571 Chemical Structure

CAS No. : 115104-28-4

Size	Price	Stock	Quantity
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 96	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 216	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 384	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 580	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 24 publication(s) in Google Scholar

Other Forms of MK-571:

MK-571 sodium In-stock

24 Publications Citing Use of MCE MK-571

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View All Isoforms

LTB₄ LTC₄/CysLT₂ LTD₄/CysLT₁ LTE₄

View All LPL Receptor Isoform Specific Products:

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LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

Biological Activity
Purity & Documentation
References
Customer Review

Description

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)

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]

In Vitro

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

MedChemExpress (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.

In Vivo

MK-571 (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 (0-1 mg/kg, orally, once) blocks LTD₄- and Ascaris-induced bronchoconstriction in conscious squirrel monkeys^[1].
MK-571 (0-25 mg/kg, orally, daily, for 2 more weeks) shows reversal of hypoxic pulmonary hypertension (PH), and protects mice from hypoxic PH^[2].

MedChemExpress (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.

Molecular Weight

515.09

Formula

C₂₆H₂₇ClN₂O₃S₂

CAS No.

115104-28-4

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(O)CCSC(C1=CC=CC(/C=C/C2=NC3=CC(Cl)=CC=C3C=C2)=C1)SCCC(N(C)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility

In Vitro:

DMSO : 175 mg/mL (339.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

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

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.66%

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Data Sheet (278 KB) SDS (393 KB)

COA (248 KB) HNMR (281 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

MK-571 Related Classifications

Inflammation/Immunology

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.

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MK-571 (Synonyms: L-660711)

Customer Review

Other Forms of MK-571:

MK-571 Related Antibodies

24 Publications Citing Use of MCE MK-571

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References

Customer Review

MK-571 Related Antibodies

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Complete Stock Solution Preparation Table

MK-571 Related Classifications

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