2. GPCR/G Protein
  3. Leukotriene Receptor LPL Receptor
  4. MK-571

MK-571 (L-660711) 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 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release.

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MK-571 Chemical Structure

MK-571 Chemical Structure

CAS No. : 115104-28-4

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Based on 24 publication(s) in Google Scholar

Other Forms of MK-571:

MK-571 Related Antibodies

Top Publications Citing Use of Products

View All Leukotriene Receptor Isoform Specific Products:

View All Isoforms
LTB4 LTC4/CysLT2 LTD4/CysLT1 LTE4

View All LPL Receptor Isoform Specific Products:

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LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

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Description

MK-571 (L-660711) 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 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release[1][2][3].

IC50 & Target[1]

LTD4

0.22 nM (Ki, In guinea pig lung)

LTD4

2.1 nM (Ki, In human lung)

LTD4

10.5 (pA2, on guinea pig ileum)

LTE4

10.4 (pA2, on guinea pig ileum)

In Vitro

MK571 (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.

MK-571 Related Antibodies

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 (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 (0-1 mg/kg, orally, once) blocks LTD4- and Ascaris-induced bronchoconstriction in conscious squirrel monkeys[1].
MK-571 (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

515.09

Formula

C26H27ClN2O3S2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(O)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, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 175 mg/mL (339.75 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 1.9414 mL 9.7070 mL 19.4141 mL
5 mM 0.3883 mL 1.9414 mL 3.8828 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9414 mL 9.7070 mL 19.4141 mL 48.5352 mL
5 mM 0.3883 mL 1.9414 mL 3.8828 mL 9.7070 mL
10 mM 0.1941 mL 0.9707 mL 1.9414 mL 4.8535 mL
15 mM 0.1294 mL 0.6471 mL 1.2943 mL 3.2357 mL
20 mM 0.0971 mL 0.4854 mL 0.9707 mL 2.4268 mL
25 mM 0.0777 mL 0.3883 mL 0.7766 mL 1.9414 mL
30 mM 0.0647 mL 0.3236 mL 0.6471 mL 1.6178 mL
40 mM 0.0485 mL 0.2427 mL 0.4854 mL 1.2134 mL
50 mM 0.0388 mL 0.1941 mL 0.3883 mL 0.9707 mL
60 mM 0.0324 mL 0.1618 mL 0.3236 mL 0.8089 mL
80 mM 0.0243 mL 0.1213 mL 0.2427 mL 0.6067 mL
100 mM 0.0194 mL 0.0971 mL 0.1941 mL 0.4854 mL
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MK-571 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

MK-571115104-28-4L-660711MK571MK 571L660711L 660711Leukotriene ReceptorLPL ReceptorLysophospholipid ReceptorRBL-2H3 cellshuman mast cellsLAD2Sphingolipidssphingosine kinaseATP-binding cassettebronchoconstrictiondyspneapulmonary hypertensionInhibitorinhibitorinhibit

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