MK-571 sodium salt hydrate (Synonyms: L-660711) |
| Catalog No.GC14980 |
Hidrato de sal de sodio MK-571, como antagonista potente y específico de la acción de los leucotrienos D4, utilizado para el tratamiento del asma.
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Cas No.: 115103-85-0
Sample solution is provided at 25 µL, 10mM.
MK-571 sodium salt hydrate, as a potent and specific antagonist of leukotriene D4 action, used for treatment of asthma[1].
In vitro test it shown that with 0.01-100 µM MK-571 reduced the export of 3H-S1P from erythrocytes in a concentration-dependent manner[2]. In vitro efficacy test it exhibited that 12.5-50 µM MK-571 in both aortic and brain derived ECs has more obvious supress-the efflux of agents rate than that of verapamil[3]. MK-571 has inhibition against LTC4 transport with IC50 of 1.0 µM[4].
In vivo, treatment with 8-32 mg/kg MK-571 intravenously in mice caused dose-dependent protection against acetic-acid-induced abdominal constriction with ED50 of 30 mg/kg[5]. In vivo, mice were instilled after endotoxin instillation at doses of 15, 35, or 50 mg/kg, MK-571 obviously inhibited the influx of inflammatory cells and reduced pro-inflammatory cytokines in BALF in a dose-dependent manner[6]. In addition, 10 ug/eye completely inhibited in vivo chemotactic responses to LTD4, and partially inhibited (54%) the responses to ovalbumin[7]. In vivo, pretreatment with 1 mg/kg MK-571 orally markedly inhibited the OA(ovalbumin)-induced EO (eosinophils) migration[8] . Treatment with 1 mg/kg/day MK-571 for at least 1 day after injury in a model of balloon catheter injury of rat carotid artery, MK-571 had effective inhibition of myointimal VSMC (vascular smooth muscle cell) proliferation, with a 58% reduction of 5-bromo-2'-deoxyuridine (BrdU) uptake in the neointima and 69% reduction of neointimal thickening[9].
References:
[1] Tocco DJ, et al. Interspecies differences in stereoselective protein binding and clearance of MK-571. Drug Metab Dispos. 1990 Jul-Aug;18(4):388-92.
[2] Christensen PM, et al. Apolipoprotein M mediates sphingosine-1-phosphate efflux from erythrocytes. Sci Rep. 2017 Nov 8;7(1):14983.
[3] Eilers M, et al. MRP (ABCC) transporters-mediated efflux of anti-HIV drugs, saquinavir and zidovudine, from human endothelial cells. Exp Biol Med (Maywood). 2008 Sep;233(9):1149-60.
[4] Schaub T, et al. ATP-dependent leukotriene export from mastocytoma cells. FEBS Lett. 1991 Feb 11;279(1):83-6.
[5] Gök S, et al. The antinociceptive effect of leukotriene D(4) receptor antagonist, MK-571, in mice: possible involvement of opioidergic mechanism. Eur J Pharmacol. 1999 Dec 15;386(2-3):195-200.
[6] Hao Q, et al. Mesenchymal Stem Cell-Derived Extracellular Vesicles Decrease Lung Injury in Mice. J Immunol. 2019 Oct 1;203(7):1961-1972.
[7] Chan CC, et al. Eosinophil-eicosanoid interactions: inhibition of eosinophil chemotaxis in vivo by a LTD4-receptor antagonist. Eur J Pharmacol. 1990 Dec 4;191(3):273-80.
[8] Foster A, et al. Peptide leukotriene involvement in pulmonary eosinophil migration upon antigen challenge in the actively sensitized guinea pig. Int Arch Allergy Appl Immunol. 1991;96(3):279-84.
[9] Porreca E, et al. Cysteinyl leukotriene D4 induced vascular smooth muscle cell proliferation: a possible role in myointimal hyperplasia. Thromb Haemost. 1996 Jul;76(1):99-104.
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