MK571

Catalog No.S8126 Synonyms: L-660711, L660711, MK-571, MK 571

MK571 Chemical Structure

Molecular Weight(MW): 537.07

MK-571 is a selective, orally active CysLT1 receptor(Cysteinyl leukotriene receptor) antagonist.

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1 Customer Review

  • The effects of verapamil (MDR1 inhibitor) and MK571 (MRP1 inhibitor) on the efflux of 5-CF at 37oC was determined by flow cytometry (B)

    Exp Hematol, 2017, 52:65-71. MK571 purchased from Selleck.

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Biological Activity

Description MK-571 is a selective, orally active CysLT1 receptor(Cysteinyl leukotriene receptor) antagonist.
Targets
CysLT1 [1] MRP1 [2] MRP4 [2] cMOAT [4]
In vitro

L-660,711 inhibited [3H]LTD4 binding in guinea pig lung with a Ki value of 0.22±0.15 nM (n=35) and [3H]LTD4 binding in human lung with a Ki value of 2.1±1.8 nM (n=29). L660,711 was essentially inactive versus [3H]LTC4 binding with IC50 values of 23±11 μM (n=16) and 32 μM (n=1) in guinea pig and human lung, respectively[1].

In vivo MK-571 is well tolerated in healthy young men. After oral administration, MK-571 is rapidly absorbed. The maximum plasma concentration occurring at 1.1-1.5 h at all doses[3].

Protocol

Cell Research:

[2]

+ Expand
  • Cell lines: Glioblastoma cell lines(U251, MZ-256, and MZ-327)
  • Concentrations: 25 µM
  • Incubation Time: 7 h
  • Method:

    Cells were seeded onto 96 well plates at a concentration of 1×103 cells per well and incubated for 72 h at 37◦C and 5% CO2 to allow MRP1 messenger RNA suppression to occur. Cells were then treated with either control media or one of three chemotherapy drugs temozolomide (150 µM), vincristine (100 nM), or etoposide (2 µM). Cells were then returned to the incubator for a further 72 h; after which time, Metylthiazol Tetrazolium (MTT) powder in PBS (50µl of 5 mg/ml) was added to each well. Cells were then incubated for a further 4 h after which all solution was removed and dimethyl sulfoxide (DMSO) was added. After 10 min incubation time at 37◦C, absorbance was recorded at 570 nm wavelength and data was recorded and analyzed. Small molecule inhibitors MK571 (25 µM) and Reversan (15µM) were added 7 h prior to carrying out further drug treatment (temozolomide, vincristine or etoposide) or assay assessment (media change for proliferation and 2D-migration assays)


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Male Msueley strain guinea pigs
  • Formulation: Saline
  • Dosages: 0.001-3.0 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (186.19 mM)
Ethanol 19 mg/mL (35.37 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 537.07
Formula

C26H27ClN2O3S2.Na

CAS No. 115103-85-0
Storage powder
Synonyms L-660711, L660711, MK-571, MK 571

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID