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编 号:F298596
分子式:C27H29N5O5
分子量:503.55
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
MRS-1706 is a potent and selective adenosine A2B receptor inverse agonist. MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1 and A3 receptors respectively. MRS-1706 blocks adenosine-mediated cAMP induction.

体内研究:
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.Animal Model:Ada–/–mice
Dosage:1 and 10 μM
Administration:Intracavernous injection
Result:Inhibited A2BR signaling and reduced the magnitude and duration.Inhibited the level of cAMP.

体外研究:
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.
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