MRS1177

MRS1177是人类腺苷A3受体(hA3AR)有效的、选择性拮抗剂，其Ki值为0.3nM。

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Background

MRS1177 is a potent and selective human Adenosine A3 receptor (hA3AR) antagonist, with a Ki of 0.3 nM.

MRS1177 (compound 2b) is a potent and selective human Adenosine A3 receptor (hA3AR) antagonist[1]. The Ki value of MRS1177 (compound 55) with hA3AR is 0.3 nM[2].

[1]. Tafi A, et al. Pharmacophore based receptor modeling: the case of adenosine A3 receptor antagonists. An approach to the optimization of protein models. J Med Chem. 2006 Jul 13;49(14):4085-97. [2]. Cheong SL, et al. Pharmacophore elucidation for a new series of 2-aryl-pyrazolo-triazolo-pyrimidines as potent human A3 adenosine receptor antagonists. Bioorg Med Chem Lett. 2011 May 15;21(10):2898-905.