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Submit ReviewMK 571
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
Purity: ≥98% (HPLC)
Biological Activity for MK 571
MK 571 is a 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 for MK 571
| M. Wt | 515.09 |
| Formula | C26H27ClN2O3S2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for MK 571
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 51.51 | 100 |
Preparing Stock Solutions for MK 571
The following data is based on the product molecular weight 515.09. Batch specific molecular weights may vary from batch to batch due to the degree 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 for MK 571
References for MK 571
References are publications that support the biological activity of the product.
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
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Keywords: MK 571, 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, 2338, Tocris Bioscience
5 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
Schnúr et al (2019) Phosphorylation-dependent modulation of CFTR macromolecular signalling complex activity by cigarette smoke condensate in airway epithelia. Sci Rep 9 12706 PMID: 31481727
Wright et al (2019) Pranlukast is a novel small molecule activator of the two-pore domain potassium channel TREK2. Biochem Biophys Res Commun 520 35 PMID: 31564414
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
Do you know of a great paper that uses MK 571 from Tocris? Please let us know.
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