|MK-571 sodium salt hydrate Catalog No.GC14980|
Sample solution is provided at 25 µL, 10mM.
GlpBio Products Cited In Reputable Papers
MiceThe Mrp4-/- mice are used. Concerning the PH reversal study, 5-week-old WT mice are maintained in hypoxia for 3 weeks, then are randomized to receive, for 2 weeks, oral vehicle or MK-571 at the doses of either 5 mg/kg/d or 25 mg/kg/d. At the same time, the experiment is designed for mice in normoxia conditions. Increased hematocrit valuesare checked to assess the efficiency of hypoxia.
. Jones TR, 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.
|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||≥ 33 mg/mL in DMSO||Storage||Store at -20°C|
|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.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
MK571 sodium salt is a specific CysLT1 (Cysteinyl-Leukotriene Type 1 Receptor) antagonist .
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 .
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 .
. 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.
. 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.
. 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.