Home Immunology & Inflammation LTR antagonist MK571 For research use only.

MK571

Synonyms: L-660711

MK571 is a selective, orally active CysLT1 receptor(Cysteinyl leukotriene receptor) antagonist.

MK571 Chemical Structure

MK571 Chemical Structure

CAS: 115104-28-4

Selleck's MK571 has been cited by 12 Publications

2 Customer Reviews

Purity & Quality Control

Batch: S812601 DMSO] 100 mg/mL] false] Ethanol] 19 mg/mL] false] Water] Insoluble] false Purity: 99.06%
99.06

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Biological Activity

Description MK571 is a selective, orally active CysLT1 receptor(Cysteinyl leukotriene receptor) antagonist.
Targets
CysLT1 [1] MRP1 [2] MRP4 [2] cMOAT [4]
In vitro
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].
Cell Research 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℃ 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)
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-MLC P2Y12 / CysLT1R / CysLT2R 23385799
In Vivo
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].
Animal Research Animal Models Male Msueley strain guinea pigs
Dosages 0.001-3.0 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 515.09 Formula

C26H27ClN2O3S2
CAS No. 115104-28-4 SDF Download MK571 SDF
Smiles CN(C)C(=O)CCSC(C1=CC=CC(=C1)C=CC2=NC3=C(C=CC(=C3)Cl)C=C2)SCCC(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (194.14 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 19 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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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