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Submit ReviewMK 571 is a potent CysLT1 (LTD4) leukotriene receptor inverse agonist (EC50 = 1.3 nM). Antagonizes LTD4-induced contractions of guinea pig trachea and ileum (pA2 values are 9.4 and 10.5 respectively). Also inhibitor of multidrug resistance protein-1 (MRP1) mediated transport; in vitro augments the effects of cytotoxic agents on malignant cells.
分子量 | 515.09 |
公式 | C26H27ClN2O3S2 |
储存 | Store at -20°C |
CAS Number | 115104-28-4 |
PubChem ID | 5281888 |
InChI Key | AXUZQJFHDNNPFG-UXBLZVDNSA-N |
Smiles | ClC1=CC=C(C=CC(/C=C/C3=CC(C(SCCC(O)=O)SCCC(N(C)C)=O)=CC=C3)=N2)C2=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 51.51 | 100 |
以下数据基于产品分子量 515.09。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.94 mL | 9.71 mL | 19.41 mL |
5 mM | 0.39 mL | 1.94 mL | 3.88 mL |
10 mM | 0.19 mL | 0.97 mL | 1.94 mL |
50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
参考文献是支持产品生物活性的出版物。
Vellenga et al (1999) Interleukin-6 production by activated human monocytic cells is enhanced by MK-571, a specific inhibitor of the multi-drug resistance protein-1. Br.J.Pharmacol. 127 441 PMID: 10385244
Dupre et al (2004) Inverse agonist activity of selected ligands of the cysteinyl-leukotriene receptor 1. J.Pharmacol.Exp.Ther. 309 102 PMID: 14718577
Blain and Sirois (2000) Involvement of LTD4 in allergic pulmonary inflammation in mice: modulation by cysLT1 antagonist MK-571. Prost.Leuko.Essent.Fatty Acids 62 361
If you know of a relevant reference for MK 571, please let us know.
关键词: MK 571, MK 571 supplier, Potent, CysLT1, LTD4, inverse, agonists, MRP, inhibitors, inhibits, Receptors, leukotrienes, eicosanoids, MDR, Resistance, Protein, Multidrug, Transporters, MK571, L660711, L-660711, Leukotriene, and, Related, 2338, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 MK 571 的部分引用包括:
Wright et al (2019) Pranlukast is a novel small molecule activator of the two-pore domain potassium channel TREK2. Biochem Biophys Res Commun 520 35 PMID: 31564414
Stott et al (2015) A primary fish gill cell culture model to assess pharmaceutical uptake and efflux: evidence for passive and facilitated transport. Antimicrob Agents Chemother 159 127 PMID: 25544062
Hoque et al (2015) Raltegravir permeability across blood-tissue barriers and the potential role of drug efflux transporters. Biochem Pharmacol 59 2572 PMID: 25691630
Hill et al (2013) Characterisation of the roles of ABCB1, ABCC1, ABCC2 and ABCG2 in the transport and pharmacokinetics of actinomycin D in vitro and in vivo. Am J Physiol Heart Circ Physiol 85 29 PMID: 23063411
Schnúr et al (2019) Phosphorylation-dependent modulation of CFTR macromolecular signalling complex activity by cigarette smoke condensate in airway epithelia. Sci Rep 9 12706 PMID: 31481727
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