MRS-1706

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 是一种有效的选择性腺苷 A2B 受体反向激动剂。

MRS-1706 has Ki values of 1.39, 112, 157, and 230 nM for human A2B, A2A, A1, and A3 receptors respectively. MRS-1706 is an effective and selective adenosine A2B receptor inverse agonist.

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.

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.

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Apoptosis

Adenosine Receptor

A1|A2A|A2B|A3

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264622-53-9

503.55

C27H29N5O5

>98% (HPLC)

DMSO:6.4 mg/mL (12.71 mM; Need ultrasonic and warming);H2O:< 0.1 mg/mL (insoluble)

O=C(NC1=CC=C(C(C)=O)C=C1)COC2=CC=C(C3=NC(N(CCC)C(N(CCC)C4=O)=O)=C4N3)C=C2

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(-20℃)

With Ice Pack

≥ 2 years