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CAS No. : 264622-53-9
MCE 国际站:MRS-1706
产品活性:MRS-1706 是一种有效选择的 A2B 腺苷受体的反向激动剂。MRS-1706 对人 A2B、A2A、A1 和 A3 受体的 Ki 值分别为 1.39、112、157 和 230 nM。MRS-1706 阻断腺苷介导的诱导 cAMP 产生。
研究领域:GPCR/G Protein
作用靶点:Adenosine Receptor
In Vitro: MRS-1706 (0.1-5 μM) has antagonist effect of NECA on the wild-type adenosine A2B receptor in a dose-dependent manner.
MRS-1706 (0.1-10000 nM) induces inhibition of yeast growth, which yeast cells expressing seven CAM adenosine A2B receptors, with IC50 values of 43, 54, 40, 98, 166, 133 nM for F84L, F84S, F84L/S95G, T42A, T42A/V54A, N36S/T42A, respectively.
MRS-1706 (1 μM) inhibits the adenosine-mediated induction of cAMP in wild-type corpus cavernosal strips (CCSs) and decreases the level of cAMP.
In Vivo: MRS-1706 (1-10 μM; intracavernous injection; Ada–/– mice) reduces the magnitude and duration of electrical field stimulation (EFS)-induced contraction of corpus cavernosal strips (CCSs) from sickle cell disease (SCD) transgenic mice and inhibits the level of cAMP.
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