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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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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MK-571 Related Classifications

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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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