MK571

Catalog No.S8126 Batch:S812601

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Technical Data

Formula

C26H27ClN2O3S2
Molecular Weight 515.09 CAS No. 115104-28-4
Solubility (25°C)* In vitro DMSO 100 mg/mL (194.14 mM)
Ethanol 19 mg/mL (36.88 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
0.41mg/ml Taking the 1 mL working solution as an example, add 50 μL of 8.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 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 (from reference)

Cell Assay:

[2]
  • 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)
Animal Study:

[1]
  • Animal Models

    Male Msueley strain guinea pigs

  • Dosages

    0.001-3.0 mg/kg

  • Administration

    i.v.

Customer Product Validation

Data from [Data independently produced by , , Eur J Pharm Sci, 2017, 106:313-327]

Data from [Data independently produced by , , Exp Hematol, 2017, 52:65-71]

Selleck's MK571 has been cited by 12 publications

Establishment and Molecular Characterization of an In Vitro Model for PARPi-Resistant Ovarian Cancer [ Cancers (Basel), 2023, 15(15)3774] PubMed: 37568590
The Modern Day Heracles: Patient-derived Liver Organoids to Model Rare Pediatric Liver Diseases [ DSpace, 2023, 10.33540/2012] PubMed: none
Transport and Permeation Properties of Dapivirine: Understanding Potential Drug-Drug Interactions [ Pharmaceutics, 2022, 14(9)1948] PubMed: 36145696
A Histone Deacetylase Inhibitor Induces Acetyl-CoA Depletion Leading to Lethal Metabolic Stress in RAS-Pathway Activated Cells [ Cancers (Basel), 2022, 14(11)2643] PubMed: 35681624
ABCC5 facilitates the acquired resistance of sorafenib through the inhibition of SLC7A11-induced ferroptosis in hepatocellular carcinoma [ Neoplasia, 2021, 23(12):1227-1239] PubMed: 34768109
Effect of prednisolone pre-treatment on cat lymphoma cell sensitivity towards chemotherapeutic drugs [ Res Vet Sci, 2021, 138:178-187] PubMed: 34157499
A thiol-bound drug reservoir enhances APR-246-induced mutant p53 tumor cell death [ EMBO Mol Med, 2020, e10852] PubMed: 33314700
In vitro Transport Ability of ABCC2 (G1249A) Polymorphic Variant Towards Anticancer Drugs. [ Onco Targets Ther, 2020, 13:1413-1419] PubMed: 32110040
LDHA Suppression Altering Metabolism Inhibits Tumor Progress by an Organic Arsenical. [ Int J Mol Sci, 2019, 20(24)] PubMed: 31835667
ES2 enhances the efficacy of chemotherapeutic agents in ABCB1-overexpressing cancer cells in vitro and in vivo [Fang Y Pharmacol Res, 2018, 129:388-399] PubMed: 29122696

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.