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MK-571 sodium salt hydrate

现货
Catalog No.
B8031
CysLT1受体拮抗剂
组合的产品项目
规格价格库存 数量
5mg
¥ 560.00
Ship with 10-15 days
10mg
¥ 980.00
Ship with 10-15 days
50mg
¥ 4,380.00
Ship with 10-15 days

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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.

文献引用

1. 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
2.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.
3. 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

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt537.07 (anhydrous basis)
Cas No.115103-85-0
FormulaC26H26ClN2NaO3S2·xH2O
SynonymsL-660711
Solubility<1.07mg/mL in DMSO, <1.164mg/mL in EtOH
Chemical Name5-(3-(2-(7-Chloroquinolin-2-yl)ethenyl)phenyl)-8-dimethylcarbamyl-4,6-dithiaoctanoic acid sodium salt hydrate
SDFDownload SDF
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

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化学结构

MK-571 sodium salt hydrate

相关生物数据

MK-571 sodium salt hydrate

相关生物数据

MK-571 sodium salt hydrate

相关生物数据

MK-571 sodium salt hydrate