CAS:264622-58-4MRS 1754

MRS 1754 is a selective adenosine A2B receptor antagonist with Ki of 1.97 nM for hA2B.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

264622-58-4

储存条件

分子式

C26H26N6O4

运输

蓝冰

分子量

486.52

别名

溶解度

DMSO	15.0 mg/mL (30.8 mM) warming
Water	Insoluble

动物实验配方

生物活性

描述The A_2B adenosine receptor (AR) is a member of the P₁ family of seven-transmembrane ARs, and it couples to G_s to increase cAMP and G_q11 to increase (1,4,5)inositol triphosphate (IP₃)/diacylglycerol (DAG). MRS 1754 is a selective antagonist ligand of A_2BAR with K_i value of 1.97 nM^[1]. ³H-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 A_2B receptor^[2]. Finally, MRS 1754 inhibited the NECA-induced Ca²⁺ 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 A_2B antagonist MRS 1754^[3].