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Stereochemistry RACEMIC
Molecular Formula C26H27ClN2O3S2
Molecular Weight 515.087
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 1
Charge 0

Structure of MK-571






Molecular Formula C26H27ClN2O3S2
Molecular Weight 515.087
Charge 0
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 1
Optical Activity ( + / - )

MK-571 is a selective, orally active leukotriene D4/E4 (LTD4/E4) receptor antagonist patented by Merck Frosst Canada, Inc. for the treatment bronchoconstriction. In ex vivo models MK-571 competitively antagonizes contractions of guinea pig trachea and ileum induced by leukotriene (LT) D4 and LTE4 and contractions of human trachea induced by LTD4. MK-571 antagonizes bronchoconstriction induced in anesthetized guinea pigs by i.v. LTC4, LTD4, and LTE4 but do not block bronchoconstriction to arachidonic acid. In clinical trials, MK-571 is a potent antagonist of LTD4-induced bronchoconstriction in both normal volunteers and asthmatic patients.

Approval Year



Primary TargetPharmacologyConditionPotency
Target ID: Q9Y271
Gene ID: 10800.0
Gene Symbol: CYSLTR1
Target Organism: Homo sapiens (Human)
22.0 nM [EC50]
Target ID: P08183
Gene ID: 5243.0
Gene Symbol: ABCB1
Target Organism: Homo sapiens (Human)


Effect of the leukotriene receptor antagonist MK-0679 on baseline pulmonary function in aspirin sensitive asthmatic subjects.
1993 Dec
Characterization of the leukotriene D4 receptor in dimethylsulphoxide-differentiated U937 cells: comparison with the leukotriene D4 receptor in human lung and guinea-pig lung.
1993 Feb 15
Leukotriene D4-induced increases in cytosolic calcium in THP-1 cells: dependence on extracellular calcium and inhibition with selective leukotriene D4 receptor antagonists.
1994 Jun
Adenosine triphosphate-dependent transport of anionic conjugates by the rabbit multidrug resistance-associated protein Mrp2 expressed in insect cells.
1998 Jun
Functional expression of the multidrug resistance protein 1 in microglia.
2003 Oct
Inverse agonist activity of selected ligands of the cysteinyl-leukotriene receptor 1.
2004 Apr
Structural requirements for the flavonoid-mediated modulation of glutathione S-transferase P1-1 and GS-X pump activity in MCF7 breast cancer cells.
2004 Apr 15
Identification of multidrug resistance-associated protein 1 and glutathione as multidrug resistance mechanisms in human prostate cancer cells: chemosensitization with leukotriene D4 antagonists and buthionine sulfoximine.
2004 Jun
Substrates and inhibitors of efflux proteins interfere with the MTT assay in cells and may lead to underestimation of drug toxicity.
2004 Oct
The human multidrug-resistance-associated protein MRP1 mediates ATP-dependent transport of unconjugated bilirubin.
2004 Oct 15
Determination of the investigational anti-cancer drug 5,6-dimethylxanthenone-4-acetic acid and its acyl glucuronide in Caco-2 monolayers by liquid chromatography with fluorescence detection: application to transport studies.
2004 Sep 25
Expression and activity of multidrug resistance protein 1 in a murine thymoma cell line.
2005 Apr
Interactions of mefloquine with ABC proteins, MRP1 (ABCC1) and MRP4 (ABCC4) that are present in human red cell membranes.
2005 Aug 15
Modulation of MRP1 protein transport by plant, and synthetically modified flavonoids.
2005 Aug 26
Inhibitory activity of a green tea extract and some of its constituents on multidrug resistance-associated protein 2 functionality.
2005 Feb
MRP-1 expression levels determine strain-specific susceptibility to sodium arsenic-induced renal injury between C57BL/6 and BALB/c mice.
2005 Feb 15
Endogenous thiols and MRP transporters contribute to Hg2+ efflux in HgCl2-treated tubular MDCK cells.
2005 Jan 5
Effects of fibrates on human organic anion-transporting polypeptide 1B1-, multidrug resistance protein 2- and P-glycoprotein-mediated transport.
2005 Jul
Combined effects of GSTP1 and MRP1 in melanoma drug resistance.
2005 Jul 25
Mrp2/Abcc2 transport activity is stimulated by protein kinase Calpha in a baculo virus co-expression system.
2005 Jun 17
Catfish egg lectin causes rapid activation of multidrug resistance 1 P-glycoprotein as a lipid translocase.
2005 Mar
Modulatory effects of plant phenols on human multidrug-resistance proteins 1, 4 and 5 (ABCC1, 4 and 5).
2005 Sep
Inhibition of MRP1-mediated efflux in human erythrocytes by mono-anionic bile salts.
2005 Sep-Oct
Involvement of P-glycoprotein and MRP1 in resistance to cyclic tetrapeptide subfamily of histone deacetylase inhibitors in the drug-resistant osteosarcoma and Ewing's sarcoma cells.
2006 Jan 1
Pharmacological inhibition of leukotrienes in an animal model of bleomycin-induced acute lung injury.
2006 Nov 21
Glutathione depletion is necessary for apoptosis in lymphoid cells independent of reactive oxygen species formation.
2007 Oct 19
Role of proline 1150 in functional interactions between the membrane spanning domains and nucleotide binding domains of the MRP1 (ABCC1) transporter.
2008 Apr 15
Cysteinyl leukotrienes mediate the enhancing effects of indomethacin and aspirin on eosinophil production in murine bone marrow cultures.
2008 Feb
A novel arsenical has antitumor activity toward As2O3-resistant and MRP1/ABCC1-overexpressing cell lines.
2008 Oct
Montelukast is a potent and durable inhibitor of multidrug resistance protein 2-mediated efflux of taxol and saquinavir.
2009 Dec
CYP1A1 induction and CYP3A4 inhibition by the fungicide imazalil in the human intestinal Caco-2 cells-comparison with other conazole pesticides.
2009 Feb 10
Cross-functioning between the extraneuronal monoamine transporter and multidrug resistance protein 1 in the uptake of adrenaline and export of 5-(glutathion-S-yl)adrenaline in rat cardiomyocytes.
2009 Jan
ABCC1, ABCC2 and ABCC3 are implicated in the transepithelial transport of the myco-estrogen zearalenone and its major metabolites.
2009 Oct 28
Culture period-dependent change of function and expression of ATP-binding cassette transporters in Caco-2 cells.
2009 Sep
Multidrug resistance protein transporter and Ins(1,4,5)P₃-sensitive Ca²+-signaling involved in adenosine triphosphate export via Gq protein-coupled NK₂-receptor stimulation with neurokinin A.
MRP transporters as membrane machinery in the bradykinin-inducible export of ATP.
2010 Apr
Chrysin blocks topotecan-induced apoptosis in Caco-2 cells in spite of inhibition of ABC-transporters.
2010 Aug 15
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
2010 Dec
Multidrug resistance proteins restrain the intestinal absorption of trans-resveratrol in rats.
2010 Mar
Differential disposition of chenodeoxycholic acid versus taurocholic acid in response to acute troglitazone exposure in rat hepatocytes.
2011 Apr
Multidrug resistance-associated protein 1 mediates 15-deoxy-Δ(12,14)-prostaglandin J2-induced expression of glutamate cysteine ligase expression via Nrf2 signaling in human breast cancer cells.
2011 Aug 15
Molecular characterization and functions of zebrafish ABCC2 in cellular efflux of heavy metals.
2011 May
Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11).
2013 Dec
The role of efflux transporters on the transport of highly toxic aconitine, mesaconitine, hypaconitine, and their hydrolysates, as determined in cultured Caco-2 and transfected MDCKII cells.
2013 Feb 4
Transcellular transport of aconitine across human intestinal Caco-2 cells.
2013 Jul
Arsenate accumulation and arsenate-induced glutathione export in astrocyte-rich primary cultures.
2013 Jun
Multidrug resistance protein 1 (ABCC1) confers resistance to arsenic compounds in human myeloid leukemic HL-60 cells.
2013 Jun
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
2013 Nov
Utilization of human nuclear receptors as an early counter screen for off-target activity: a case study with a compendium of 615 known drugs.
2015 Jun
Nrf2 Regulates the Sensitivity of Mouse Keratinocytes to Nitrogen Mustard via Multidrug Resistance-Associated Protein 1 (Mrp1).
2016 Jan


Sample Use Guides

1,500, 86, or 28 mg
Route of Administration: Intravenous
Substance Class Chemical
by admin
on Wed Jul 05 23:25:48 UTC 2023
by admin
on Wed Jul 05 23:25:48 UTC 2023
Record UNII
Record Status Validated (UNII)
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Name Type Language
Common Name English
Code English
Common Name English
MK 571
Code English
Code English
Common Name English
L 660711
Code English
Common Name English
Code System Code Type Description
Created by admin on Wed Jul 05 23:25:48 UTC 2023 , Edited by admin on Wed Jul 05 23:25:48 UTC 2023
EPA CompTox
Created by admin on Wed Jul 05 23:25:48 UTC 2023 , Edited by admin on Wed Jul 05 23:25:48 UTC 2023
Created by admin on Wed Jul 05 23:25:48 UTC 2023 , Edited by admin on Wed Jul 05 23:25:48 UTC 2023
Created by admin on Wed Jul 05 23:25:48 UTC 2023 , Edited by admin on Wed Jul 05 23:25:48 UTC 2023
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