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MRS1523
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MRS1523图片
CAS NO:212329-37-8
包装与价格:
包装价格(元)
1mg (solution)电议
5mg (solution)电议
10mg (solution)电议
25mg (solution)电议

产品介绍

化学性质

Physical AppearanceA solution in ethanol. To change the solvent, simply evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice.
StorageSupplied as a solution in ethanol,Store at -20°C
M.Wt399.5
Cas No.212329-37-8
FormulaC23H29NO3S
Solubility≤50mg/ml in DMSO;50mg/ml in dimethyl formamide
Chemical Name6-ethyl-5-[(ethylthio)carbonyl]-2-phenyl-4-propyl-3-pyridinecarboxylic acid propyl ester
Canonical SMILESCCCOC(C1=C(CCC)C(C(SCC)=O)=C(CC)N=C1C2=CC=CC=C2)=O
运输条件蓝冰运输或根据您的需求运输。
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。溶液形式一般不宜长期储存,请尽快用完。

资料参考

Ki = 18.9 nM for human adenosine A3 receptor

Ki = 113 nM for rat adenosine A3 receptor

MRS1523 is a selective adenosine A3 receptor (A3R) antagonist. A3R is strongly overexpressed in cancer cell lines and cancer tissues. The activation of the A3R is related to several second messenger systems which are for signaling pathways including asthmatic, inflammatory, and ischemic responses.

In vitro: MRS1523 reversed the increase in mRNA expression in B16-F10 Melanoma Cells. Also, MRS1523 antagonized the modulation in the expression level of the proteins, which indicated that adenosine A3R mediated the responses [1].

In vivo: C57BL/6J, male mice, inoculated B16-F10 melanoma cells, were administered MRS1523 at a dose of 100 μg/kg orally twice daily for 15 days. MRS1523 counteracted the activity of IB-MECA which is an adenosine A3R agonist. In addition, it was demonstrated that the response was adenosine A3R mediated. The modulation of up-regulation of GSK-3β expression level was neutralized by MRS1523, further suggesting the specificity of the response [1].

Reference:
[1].  Madi, L., Rosenberg-Haggen, B., Nyska, A., & Korenstein, R. Enhancing pigmentation via activation of A3 adenosine receptors in B16 melanoma cells and in human skin explants. Experimental Dermatology. 2012; 22(1): 74-77.