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MK-571 sodium

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Chemical Structure| 115103-85-0 同义名 : L-660711 sodium;MK-571 Sodium salt;MK-571 (sodium salt);L-660711 sodium salt;L-660711
CAS号 : 115103-85-0
货号 : A407864
分子式 : C26H26ClN2NaO3S2
纯度 : 95%
分子量 : 537.069
MDL号 : MFCD00878420
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 30 mg/mL(55.86 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Leukotrienes (LT) C4, D4s and E4 are thought to play a fundamental role in lung pathophysislogy. MK-571 Sodium is a potent and selective LTD4 receptor antagonist with Ki values of 0.22 nM and 2.1 nM in guinea pig and human lung membranes, respectively[6]. MK571 is also a multidrug resistance protein-2 (ABCC2, Mrp2) inhibitor. MK571 treatment at 25 μM showed an enhanced effect of vincristine and etoposide in reducing cell viability over a 72 h period in GBM tumor biopsy derived cell lines MZ-256 and MZ-304[7]. MK571 (50 μM, 100 μM) dose-dependently inhibited the intracellular biosynthesis of all flavonol glucuronides and sulphates by Caco-2 cells. MK571 significantly inhibited phase-2 conjugation of kaempferol by cell-free extracts of Caco-2, and production of kaempferol-40-O-glucuronide, which indicated that MK571 is a potential inhibitor of enterocyte phase-2 conjugation[8].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.86mL

0.37mL

0.19mL

9.31mL

1.86mL

0.93mL

18.62mL

3.72mL

1.86mL
参考文献

[1]Tivnan A, Zakaria Z, et al. Inhibition of multidrug resistance protein 1 (MRP1) improves chemotherapy drug response in primary and recurrent glioblastoma multiforme. Front Neurosci. 2015 Jun 16;9:218.

[2]Jones TR, Zamboni R, 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.

[3]Yang XX, Powell WS, et al. Hyperpnea-induced bronchoconstriction is dependent on tachykinin-induced cysteinyl leukotriene synthesis. J Appl Physiol (1985). 1997 Feb;82(2):538-44.

[4]Kanwar S, Johnston B, et al. Leukotriene C4/D4 induces P-selectin and sialyl Lewis(x)-dependent alterations in leukocyte kinetics in vivo. Circ Res. 1995 Nov;77(5):879-87.

[5]Kilic E, Spudich A, et al. ABCC1: a gateway for pharmacological compounds to the ischaemic brain. Brain. 2008 Oct;131(Pt 10):2679-89.

[6]Jones TR, Zamboni R, Belley M, Champion E, Charette L, Ford-Hutchinson AW, Frenette R, Gauthier JY, Leger S, Masson P, 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. doi: 10.1139/y89-004. PMID: 2540892.

[7]Tivnan A, Zakaria Z, O'Leary C, Kögel D, Pokorny JL, Sarkaria JN, Prehn JH. Inhibition of multidrug resistance protein 1 (MRP1) improves chemotherapy drug response in primary and recurrent glioblastoma multiforme. Front Neurosci. 2015 Jun 16;9:218. doi: 10.3389/fnins.2015.00218. PMID: 26136652; PMCID: PMC4468867.

[8]Barrington RD, Needs PW, Williamson G, Kroon PA. MK571 inhibits phase-2 conjugation of flavonols by Caco-2/TC7 cells, but does not specifically inhibit their apical efflux. Biochem Pharmacol. 2015 Jun 1;95(3):193-200. doi: 10.1016/j.bcp.2015.03.005. Epub 2015 Mar 20. PMID: 25801004; PMCID: PMC4428793.