MK 571

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Cat.No. 2338 - MK 571 | C26H27ClN2O3S2 | CAS No. 115104-28-4
Description: Potent CysLT1 (LTD4) inverse agonist. Also MRP1 inhibitor
Alternative Names: L-660711
Chemical Name: 3-[[[3-[(1E)-2-(7-Chloro-2-quinolinyl)ethenyl]phenyl][[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]propanoic acid
Datasheet
Citations (3)
Literature

Biological Activity

Potent CysLT1 (LTD4) leukotriene receptor inverse agonist (EC50 = 1.3 nM). Antagonizes LTD4-induced contractions of guinea pig trachea and ileum (pA2 values are 9.4 and 10.5 respectively). Also inhibitor of multidrug resistance protein-1 (MRP1) mediated transport; in vitro augments the effects of cytotoxic agents on malignant cells.

Technical Data

M. Wt 515.09
Formula C26H27ClN2O3S2
Storage Store at -20°C
CAS Number 115104-28-4
PubChem ID 5281888
InChI Key AXUZQJFHDNNPFG-UXBLZVDNSA-N
Smiles ClC1=CC=C(C=CC(/C=C/C3=CC(C(SCCC(O)=O)SCCC(N(C)C)=O)=CC=C3)=N2)C2=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 51.51 100

Preparing Stock Solutions

The following data is based on the product molecular weight 515.09. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.94 mL 9.71 mL 19.41 mL
5 mM 0.39 mL 1.94 mL 3.88 mL
10 mM 0.19 mL 0.97 mL 1.94 mL
50 mM 0.04 mL 0.19 mL 0.39 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Vellenga et al (1999) Interleukin-6 production by activated human monocytic cells is enhanced by MK-571, a specific inhibitor of the multi-drug resistance protein-1. Br.J.Pharmacol. 127 441 PMID: 10385244

Dupre et al (2004) Inverse agonist activity of selected ligands of the cysteinyl-leukotriene receptor 1. J.Pharmacol.Exp.Ther. 309 102 PMID: 14718577

Blain and Sirois (2000) Involvement of LTD4 in allergic pulmonary inflammation in mice: modulation by cysLT1 antagonist MK-571. Prost.Leuko.Essent.Fatty Acids 62 361 PMID:


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View Related Products by Product Action

View all Leukotriene and Related Receptor Antagonists

Keywords: MK 571, supplier, Potent, CysLT1, LTD4, inverse, agonists, MRP, inhibitors, inhibits, Receptors, leukotrienes, eicosanoids, MDR, Resistance, Protein, Multidrug, Transporters, MK571, L660711, L-660711, Leukotriene, and, Related, Receptors, Multidrug, Transporters, Leukotriene, and, Related, Receptors, Tocris Bioscience

3 Citations for MK 571

Citations are publications that use Tocris products. Selected citations for MK 571 include:

Hill et al (2013) Characterisation of the roles of ABCB1, ABCC1, ABCC2 and ABCG2 in the transport and pharmacokinetics of actinomycin D in vitro and in vivo. Am J Physiol Heart Circ Physiol 85 29 PMID: 23063411

Stott et al (2015) A primary fish gill cell culture model to assess pharmaceutical uptake and efflux: evidence for passive and facilitated transport. Antimicrob Agents Chemother 159 127 PMID: 25544062

Hoque et al (2015) Raltegravir permeability across blood-tissue barriers and the potential role of drug efflux transporters. Biochem Pharmacol 59 2572 PMID: 25691630


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