MRS 1754
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货号：A540042
MRS 1754 is a selective adenosine A2B receptor antagonist with Ki of 1.97 nM for hA2B.
MRS 1754 化学结构
MRS 1754 3D分子结构
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MRS 1754 纯度/质量文件 产品仅供科研
货号：A540042
标准纯度：
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产品说明书
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MRS 1754 质控信息
ZM241385
✔
99%+
Istradefylline
+++
Adenosine A2A receptor, Ki: 2.2 nM
98%
Reversine
+
human A3 adenosine receptor, Ki: 0.66 μM
98%
SCH58261
++++
bovine A2a, Ki: 2.0 nM
rat A2a, Ki: 2.3 nM
99%+
A2A receptor antagonist 1
++
A1R, Ki: 264 nM
A2AR, Ki: 4 nM
99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
MRS 1754 生物活性
描述
The A2B adenosine receptor (AR) is a member of the P1 family of seven-transmembrane ARs, and it couples to Gs to increase cAMP and Gq11 to increase (1,4,5)inositol triphosphate (IP3 )/diacylglycerol (DAG). MRS 1754 is a selective antagonist ligand of A2B AR with Ki value of 1.97 nM[1] 3 H-MRS 1754 was shown to bind with high affinity to a single class of binding sites in membranes of HEK-293 cells expressing the human A2B receptor[2] 2+ responses and cAMP production in a concentration-dependent manner. Treatment of the T24 cell line for 4h with NECA resulted in an increase in interleukin-8 production which was sensitive to the adenosine A2B antagonist MRS 1754[3]
MRS 1754 参考文献
[1] Kalla RV, Zablocki J, Tabrizi MA, Baraldi PG. Recent developments in A2B adenosine receptor ligands. Handb Exp Pharmacol . 2009;(193):99-122
[2] Ji X, Kim YC, Ahern DG, Linden J, Jacobson KA. 3 HMRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors. Biochem Pharmacol . 2001;61(6):657-663
[3] Phelps PT, Anthes JC, Correll CC. Characterization of adenosine receptors in the human bladder carcinoma T24 cell line. Eur J Pharmacol . 2006;536(1-2):28-37
MRS 1754 实验方案
计算器
摩尔计算器
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工作液计算器
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1mg
5mg
10mg
1 mM
5 mM
10 mM
2.06mL
0.41mL
0.21mL
10.28mL
2.06mL
1.03mL
20.55mL
4.11mL
2.06mL
MRS 1754 技术信息
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