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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电议
5mg电议
10mg电议
25mg电议

产品介绍
MRS1523 是一种有效的选择性腺苷 A3 受体拮抗剂,对人和大鼠 A3 受体的 Ki 值分别为 18.9 nM 和 113 nM。
Cas No.212329-37-8
化学名6-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
分子式C23H29NO3S
分子量399.5
溶解度≤50mg/ml in DMSO;50mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.