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Chemical Structure| 115103-85-0 Chemical Structure| 115103-85-0

Structure of MK-571 sodium
CAS No.: 115103-85-0

Chemical Structure| 115103-85-0

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MK-571 Sodium is a competitive, potent and selective LTD4 antagonist with Ki values of 0.22 nM.

Synonyms: L-660711 sodium; MK-571 Sodium salt; MK-571 (sodium salt)

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Product Details of MK-571 sodium

CAS No. :115103-85-0
Formula : C26H26ClN2NaO3S2
M.W : 537.07
SMILES Code : O=C([O-])CCSC(C1=CC=CC(/C=C/C2=NC3=CC(Cl)=CC=C3C=C2)=C1)SCCC(N(C)C)=O.[Na+]
Synonyms :
L-660711 sodium; MK-571 Sodium salt; MK-571 (sodium salt)
MDL No. :MFCD00878420

Safety of MK-571 sodium

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
U937 cell line 10 μM 24 hours MK-571 enhanced IL-6 promoter activity in IL-1-stimulated U937 cells. PMC1566046
RPCEC 100 μM In rPCEC, MK-571 significantly enhanced the uptake of [3H]-cyclosporine-A and [14C]-erythromycin. PMC1995119
Caco-2 cells 50 μM 1 hour To study the effect of MK-571 on the uptake of (+)-catechin and puerarin in Caco-2 cells, results showed MK-571 significantly increased the cellular uptake of (+)-catechin and puerarin PMC4820802
Rat aortic smooth muscle cells (RASMs) 1-100 nM 10 minutes MK-571 (1-100 nM) dose-dependently reduced the LTD4-induced increase in intracellular calcium concentration, with an IC50 of approximately 3.1 nM. PMC1573698
A549 cells 25 µM 2 hours MK-571 was less effective than hydroxychalcones (HCs) in inducing intracellular GSH depletion in A549 cells PMC3983951
PC-3 cells 25 µM 24 hours MK-571 was less effective than apigenin in inducing intracellular GSH depletion in PC-3 cells PMC3983951
HL-60 cells 25 µM 24 hours MK-571 was less effective than hydroxychalcones (HCs) in inducing intracellular GSH depletion in HL-60 cells PMC3983951
Human peripheral blood monocytes 10 μM 24 hours MK-571 enhanced IL-6 expression and secretion in monocytes stimulated with LPS or IL-1. PMC1566046
Mouse G3 MB tumorspheres 5–50µM 30 minutes To assess Abcc4 function by measuring PMEA drug accumulation. Radiolabeled PMEA accumulation increased with the dose of MK571. PMC4573843
MDCKII-MRP2 cells 100 μM 30 minutes MK-571 completely inhibited MRP2-mediated efflux of Lopinavir, reducing the efflux ratio to 1.0 PMC3166960
EL4 cells 6.25, 12.5, 25 µM 30 minutes To evaluate the inhibitory effect of MK-571 on MRP1 activity, results showed that MK-571 inhibited MRP1 activity in a concentration-dependent manner. PMC1782113
K562 cells 10 μM and 30 μM 4 days MK-571 significantly increased the antiproliferative effect of bestatin on K562 cells and at 30 μM concentration also increased the effect of actinonin, indicating that these inhibitors enter the cells and their intracellular concentration is affected by MRP-mediated transport. PMC7127609
U937 cells 10 μM and 30 μM 4 days MK-571 increased the antiproliferative effects of both bestatin and actinonin on U937 cells, indicating that these inhibitors enter the cells and their intracellular concentration is affected by MRP-mediated transport. PMC7127609
Human SK-MEL-28 melanoma cells 10 µM 48 hours MK-571, a selective MRP inhibitor, when used in combination with CAPE, decreased the IC50 of CAPE (15 µM) by 13%, increased CAPE-induced apoptotic cell death by 3%, and decreased mitochondrial membrane potential by 10%. PMC3706206
EL4 cells 12.5 µM 6 days To study the effect of MK-571 on EL4 cell differentiation, results showed that MK-571 induced the expression of CD4 and CD8 molecules in EL4 cells. PMC1782113
RLFφ13 cells 10 µM and 20 µM 60 minutes To study the inhibitory effect of MK571 on Mrp activity in RLFφ13 cells, results showed that MK571 significantly inhibited Mrp-mediated substrate efflux. PMC1773728
MDCKII-MRP2 100 μM In MDCKII-MRP2 cells, MK-571 significantly enhanced the uptake of [3H]-cyclosporine-A and [14C]-erythromycin. PMC1995119
SV40-HCEC 75 μM In SV40-HCEC, MK-571 significantly enhanced the uptake of [3H]-cyclosporine-A and [14C]-erythromycin. PMC1995119

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
FVB mice Hypoxia-induced pulmonary hypertension model Oral 5 mg/kg or 25 mg/kg Once daily for 2 weeks MK571 reversed hypoxia-induced pulmonary hypertension, reduced right ventricular systolic pressure and Fulton index, and decreased vascular remodeling of small pulmonary arteries. PMC3223830

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.86mL

0.37mL

0.19mL

9.31mL

1.86mL

0.93mL

18.62mL

3.72mL

1.86mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

[1]Tivnan A, Zakaria Z, et al. Inhibition of multidrug resistance protein 1 (MRP1) improves chemotherapy drug response in primary and recurrent glioblastoma multiforme. Front Neurosci. 2015 Jun 16;9:218.

[2]Jones TR, Zamboni R, et al. Pharmacology of L-660,711 (MK-571): a novel potent and selective leukotriene D4 receptor antagonist. Can J Physiol Pharmacol. 1989 Jan;67(1):17-28.

[3]Yang XX, Powell WS, et al. Hyperpnea-induced bronchoconstriction is dependent on tachykinin-induced cysteinyl leukotriene synthesis. J Appl Physiol (1985). 1997 Feb;82(2):538-44.

[4]Kanwar S, Johnston B, et al. Leukotriene C4/D4 induces P-selectin and sialyl Lewis(x)-dependent alterations in leukocyte kinetics in vivo. Circ Res. 1995 Nov;77(5):879-87.

[5]Kilic E, Spudich A, et al. ABCC1: a gateway for pharmacological compounds to the ischaemic brain. Brain. 2008 Oct;131(Pt 10):2679-89.

[6]Jones TR, Zamboni R, Belley M, Champion E, Charette L, Ford-Hutchinson AW, Frenette R, Gauthier JY, Leger S, Masson P, et al. Pharmacology of L-660,711 (MK-571): a novel potent and selective leukotriene D4 receptor antagonist. Can J Physiol Pharmacol. 1989 Jan;67(1):17-28. doi: 10.1139/y89-004. PMID: 2540892.

[7]Tivnan A, Zakaria Z, O'Leary C, Kögel D, Pokorny JL, Sarkaria JN, Prehn JH. Inhibition of multidrug resistance protein 1 (MRP1) improves chemotherapy drug response in primary and recurrent glioblastoma multiforme. Front Neurosci. 2015 Jun 16;9:218. doi: 10.3389/fnins.2015.00218. PMID: 26136652; PMCID: PMC4468867.

[8]Barrington RD, Needs PW, Williamson G, Kroon PA. MK571 inhibits phase-2 conjugation of flavonols by Caco-2/TC7 cells, but does not specifically inhibit their apical efflux. Biochem Pharmacol. 2015 Jun 1;95(3):193-200. doi: 10.1016/j.bcp.2015.03.005. Epub 2015 Mar 20. PMID: 25801004; PMCID: PMC4428793.

 

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