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MK-571 sodium salt hydrate CysLT1 receptor antagonist

Catalog No.B8031
Size Price Stock Qty
5mg
$56.00
In stock
10mg
$98.00
In stock
50mg
$438.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

MK-571 sodium salt hydrate

MK-571 sodium salt hydrate Dilution Calculator

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Chemical Properties

Cas No. 115103-85-0 SDF Download SDF
Synonyms L-660711
Chemical Name 5-(3-(2-(7-Chloroquinolin-2-yl)ethenyl)phenyl)-8-dimethylcarbamyl-4,6-dithiaoctanoic acid sodium salt hydrate
Formula C26H26ClN2NaO3S2·xH2O M.Wt 537.07 (anhydrous basis)
Solubility Soluble in Water Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

MK571 sodium salt is a specific CysLT1 (Cysteinyl-Leukotriene Type 1 Receptor) antagonist [1].

Cysteinyl leukotriene receptor 1, also termed as CYSLTR1, is a receptor for cysteinyl leukotrienes (LT)which mediates a large variety of allergic and hypersensitivity reactions in humans [2].

In vitro: MK571 is a multidrug resistance protein-2 (ABCC2, Mrp2) inhibitor and had been widely used to demonstrate the role of Mrp2 in the cellular efflux of drugs, xenobiotics and their conjugates. Apically-applied MK571 resulted in significant reductions in both the apical and basolateral efflux of flavonol conjugates from Caco-2/TC7 monolayers. The estimated Ki for inhibition of the synthesis of K-4′-O-GlcA by MK571 is 19.7 μM. MK571 inhibited the intracellular biosynthesis of all flavonol glucuronides and sulphates by Caco-2 cells in a dose-dependent manner. MK571 significantly inhibited phase-2 conjugation of kaempferol by cell-free extracts of Caco-2, and competitively inhibited the production of kaempferol-4′-O-glucuronide. These data indicated that MK571, in addition to inhibiting MRP2, was a potential inhibitor of enterocyte phase-2 conjugation [3].

References:
[1].  Thivierge M, Turcotte S, Rola-Pleszczynski M, et al. Enhanced cysteinyl-leukotriene type 1 receptor expression in T cells from house dust mite-allergic individuals following stimulation with Der p[J]. Journal of immunology research, 2015, 2015.
[2].  Singh RK, Tandon R, Dastidar SG, Ray A (November 2013). "A review on leukotrienes and their receptors with reference to asthma". The Journal of Asthma. 50 (9): 922–31.
[3].  Barrington R D, Needs P W, Williamson G, et al. MK571 inhibits phase-2 conjugation of flavonols by Caco-2/TC7 cells, but does not specifically inhibit their apical efflux[J]. Biochemical pharmacology, 2015, 95(3): 193-200.