1. Membrane Transporter/Ion Channel GPCR/G Protein
  2. Leukotriene Receptor LPL Receptor P-glycoprotein
  3. MK-571 sodium

MK-571 sodium  (Synonyms: L-660711 sodium)

Cat. No.: HY-19989A Purity: 99.75%
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MK-571 (L-660711) sodium is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 sodium is also a inhibitor of multidrug resistance-associated protein MRP4 (ABCC4) and ABCC1 (MRP1). MK-571 sodium inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release.

For research use only. We do not sell to patients.

CAS No. : 115103-85-0

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Customer Review

Based on 33 publication(s) in Google Scholar

Other Forms of MK-571 sodium:

Top Publications Citing Use of Products

33 Publications Citing Use of MCE MK-571 sodium

Cell Proliferation/Viability Assay
Bio/Physico-chemical Assay
Cell Imaging/Staining
IF
WB
In Vivo Efficacy Study

    MK-571 sodium purchased from MedChemExpress. Usage Cited in: Toxicology. 2025 Jun 3:154210.  [Abstract]

    MK-571 (5 μM, 1 h) dilates the bile canalicular area in HepaRG cells.

    MK-571 sodium purchased from MedChemExpress. Usage Cited in: Toxicology. 2025 Jun 3:154210.  [Abstract]

    MK-571 (5 μM, 6 h) reduced the expression of NTCP, BSEP, and MRP3 in HepaRG cells.

    MK-571 sodium purchased from MedChemExpress. Usage Cited in: Sci Adv. 2024 Dec 13;10(50):eadq4274.  [Abstract]

    Cells were treated with the ABCC1 inhibitor MK-571 sodium (10 μM) and MRTX849 for 3 days, followed by CCK-8 assays. The results showed that MK-571 sodium improved the efficacy of MRTX849 in two resistant cells.

    MK-571 sodium purchased from MedChemExpress. Usage Cited in: Sci Adv. 2024 Dec 13;10(50):eadq4274.  [Abstract]

    Cells were treated with 1 μM MRTX849 for 6 hours or with 10 μM MK-571 sodium for 24 hours, followed by 1 μM MRTX849 for 6 hours. Intracellular MRTX849 accumulation was quantified using LC-MS/MS (Student’s t test). The results showed that MK-571 sodium improved the efficacy of MRTX849 in two resistant cells.

    MK-571 sodium purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2024 Jun 19:S0891-5849(24)00531-8.  [Abstract]

    HT1080 and HUH7 cells were pretreated with Verapamil (20 μM) or MK-571 sodium (40 μM) for 2 h and then treated with DMSO or RU486 (5 μM) together with concentration gradient of RSL3 (0–10 μM) for 24 h. Cell viability was measured by CCK-8 (n = 3).

    MK-571 sodium purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2024 Aug 14;10(1):364.  [Abstract]

    MK-571 (5 μM, 30 min) increased the fluorescence intensity of DOX-inducible CD10+ PTEC CMFDA metabolites.

    MK-571 sodium purchased from MedChemExpress. Usage Cited in: Cell. 2023 Dec 7;186(25):5500-5516.e21.  [Abstract]

    Survival curves for mice subjected to SD (SR means 48 h of recovery after SD) with oral administration of MK-571 sodium (0.1 mg/mL) (n = 10) in the drinking water compared with water controls (n = 10). The results showed that MK-571 sodium protected against SD-induced mortality.

    MK-571 sodium purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Sep;129:110506.  [Abstract]

    MK-571 (50 μM, 10 min) increased the accumulation of [3H]-MVC in BeWo cells.

    MK-571 sodium purchased from MedChemExpress. Usage Cited in: Arch Toxicol. 2020 Nov;94(11):3799-3817.  [Abstract]

    The MRP1 inhibitor MK-571 sodium (50 µM; 1 h) decreased A–B MeHg transport in MDCKII-MRP1 cells.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    MK-571 (L-660711) sodium is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 sodium is also a inhibitor of multidrug resistance-associated protein MRP4 (ABCC4) and ABCC1 (MRP1). MK-571 sodium inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release[1][2][3].

    IC50 & Target[1]

    LTD4

    0.22±0.15 nM (Ki, In guinea pig lung)

    LTD4

    2.1±1.8 nM (Ki, In human lung)

    LTD4

    10.5 (pA2)

    LTE4

    10.4 (pA2)

    Cellular Effect
    Cell Line Type Value Description References
    2008 IC50
    7.57 μM
    Compound: MK-571
    Inhibition of human MRP1 in human 2008 cells
    Inhibition of human MRP1 in human 2008 cells
    [PMID: 18707884]
    MDCK-II IC50
    20.7 μM
    Compound: MK-571
    Inhibition of human MRP2 expressed in dog MDCK2 cells
    Inhibition of human MRP2 expressed in dog MDCK2 cells
    [PMID: 18707884]
    MDCK-II IC50
    > 30 μM
    Compound: MK571
    Inhibition of human MRP1 transfected in MDCK2 cells assessed as inhibition of calcein-AM efflux
    Inhibition of human MRP1 transfected in MDCK2 cells assessed as inhibition of calcein-AM efflux
    [PMID: 26774038]
    In Vitro

    MK571 sodium (15 μM, 1 h) markedly suppresses constitutive and Ag-stimulated S1P secretion from RBL-2H3 cells and mast cells, and inhibits Fluo-3 efflux[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Viability Assay[3]

    Cell Line: RBL-2H3 cells, human LAD2 mast cells
    Concentration: 15 μM
    Incubation Time: 1 h
    Result: Inhibited S1P secretion by vector and SphK1 transfected RBL-2H3 cells, whereas it did not affect uptake and intracellular conversion of [3H]Sph to S1P. Inhibited Fluo-3 efflux, inhibited S1P export by LAD2 cells, and blocked Ag-stimulated release of S1P.
    In Vivo

    MK-571 sodium (0-0.5 mg/kg, orally, once) produces dose-dependent inhibition of the duration of antigen-induced dyspnea in conscious sensitized rats treated with Methysergide (3 μg/kg)[1].
    MK-571 sodium (0-1 mg/kg, orally, once) blocks LTD4- and Ascaris-induced bronchoconstriction in conscious squirrel monkeys[1].
    MK-571 sodium (0-25 mg/kg, orally, daily, for 2 more weeks) shows reversal of hypoxic pulmonary hypertension (PH), and protects mice from hypoxic PH[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Hyperreactive rats (male and female, 200-400 g, pretreated intravenously with 3 μg/kg methysergide, 5 min before antigen chdlenge)[1]
    Dosage: 0.5, 0.15, and 0.05 mg/kg
    Administration: Orally, once, 1 or 4 h before challenge
    Result: Produced dose-dependent inhibition of the duration of antigen-induced dyspnea, with ED50 values of 0.13 (95% confidence interval (CI), 0.03-0.62) and 0.11 (95% CI, 0.009-1.47) mg/kg, respectively. MK-571 was even more active when administered orally as a suspension in 1% Methocel (4 h pretreatment), with an ED50 of 0.068 (95% CI, 0.83-0.14) mg/kg.
    Animal Model: Csnscisus squirrel msnkeys[1]
    Dosage: 0.1, 0.5, and 1 mg/kg
    Administration: Orally, once, 2 h prior to challenge with Ascaris antigen
    Result: Produced significant inhibition of the bronchoconstriction at 0.5 mg/kg, produced significant inhibition of the increases in RL and decreases in Cdyn at 1 mg/kg.
    Animal Model: FVB (Friend virus B-type) mice (Mrp4–/– and WT, 6 weeks old, exposed to chronic hypoxia (10% O2) in a ventilated chamber for 28 days)[2]
    Dosage: 0, 5, and 25 mg/kg
    Administration: Orally, daily, for 2 more weeks, maintain in hypoxic conditions
    Result: Showed reversal of hypoxic pulmonary hypertension (PH), and mice were protected from hypoxic PH. MK-571-treated mice displayed lower RVSP and Fulton index and a decrease in the medial thickening of small pulmonary arteries and arterioles.
    Molecular Weight

    537.07

    Formula

    C26H26ClN2NaO3S2

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(O[Na])CCSC(C1=CC=CC(/C=C/C2=NC3=CC(Cl)=CC=C3C=C2)=C1)SCCC(N(C)C)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (93.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8620 mL 9.3098 mL 18.6195 mL
    5 mM 0.3724 mL 1.8620 mL 3.7239 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.17 mg/mL (4.04 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.17 mg/mL (4.04 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
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    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    +
    %
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    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.75%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8620 mL 9.3098 mL 18.6195 mL 46.5489 mL
    5 mM 0.3724 mL 1.8620 mL 3.7239 mL 9.3098 mL
    10 mM 0.1862 mL 0.9310 mL 1.8620 mL 4.6549 mL
    15 mM 0.1241 mL 0.6207 mL 1.2413 mL 3.1033 mL
    20 mM 0.0931 mL 0.4655 mL 0.9310 mL 2.3274 mL
    25 mM 0.0745 mL 0.3724 mL 0.7448 mL 1.8620 mL
    30 mM 0.0621 mL 0.3103 mL 0.6207 mL 1.5516 mL
    40 mM 0.0465 mL 0.2327 mL 0.4655 mL 1.1637 mL
    50 mM 0.0372 mL 0.1862 mL 0.3724 mL 0.9310 mL
    60 mM 0.0310 mL 0.1552 mL 0.3103 mL 0.7758 mL
    80 mM 0.0233 mL 0.1164 mL 0.2327 mL 0.5819 mL
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    MK-571 sodium
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