MK-571 sodium salt hydrate
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.
- 1. Mairinger S, Sake JA, et al. "Assessing the Activity of Multidrug Resistance-Associated Protein 1 at the Lung Epithelial Barrier." J Nucl Med. 2020;jnumed.120.244038. PMID:32284394
- 2. Fang Y, Cao W, et al. "Structure affinity relationship and docking studies of flavonoids as substrates of multidrug-resistant associated protein 2 (MRP2) in MDCK/MRP2 cells." Food Chem. 2019 Sep 1;291:101-109. PMID:31006447
- 3. Yi Xiao,Lei Xin,et al. "Quercetin and kaempferol increase the intestinal absorption of isorhamnetin coexisting in Elaeagnus rhamnoides (L.) A. Nelson (Elaeagnaceae) extracts via regulating multidrug resistance-associated protein 2." Phytomedicine Available online 4 September 2018.
- 4. Chee YC, Pahnke J, et al. "Intrinsic Xenobiotic Resistance of the Intestinal Stem Cell Niche." Dev Cell. 2018 Aug 21.pii: S1534-5807(18)30608-7. PMID:30146480
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 537.07 (anhydrous basis) |
Cas No. | 115103-85-0 |
Formula | C26H26ClN2NaO3S2·xH2O |
Synonyms | L-660711 |
Solubility | ≥10.3 mg/mL in DMSO with gentle warming and ultrasonic; ≥122.2 mg/mL in H2O; ≥8.3 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 5-(3-(2-(7-Chloroquinolin-2-yl)ethenyl)phenyl)-8-dimethylcarbamyl-4,6-dithiaoctanoic acid sodium salt hydrate |
SDF | Download SDF |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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