Sp-cAMPS sodium salt

• 常用名: Sp-cAMPS sodium salt
• 英文名: Sp-cAMPS sodium salt
• CAS号: 142439-95-0
• 分子量: 367.253
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₀H₁₁N₅NaO₅PS
• 熔点: N/A
• 闪点: N/A

Sp-cAMPS sodium salt用途

Sp-cAMPS sodium salt, a cAMP analog, is potent activator of cAMP-dependent PKA I 和 PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC50 of 40 μM[1][2][3].

Sp-cAMPS sodium salt名称

• 中文名: Sp-Cyclic AMPS sodium salt
• 英文名: Sodium (2S,4aR,6R,7R,7aS)-6-(6-amino-9H-purin-9-yl)-7-hydroxytetr ahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2-thiolate 2-oxide

Sp-cAMPS sodium salt生物活性

• 描述: Sp-cAMPS sodium salt,一种 cAMP 类似物,是一种依赖 cAMP 的 PKA I 和 PKA II 的有效激活剂。Sp-cAMPS sodium salt 还是一种有效的竞争性磷酸二酯酶 (PDE3A) 抑制剂,Ki 为 47.6 µM。Sp-cAMPS sodium salt 以 EC50 为 40 μM 来结合 PDE10 GAF 域。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> 磷酸二酯酶(PDE)
  信号通路 >> 蛋白酪氨酸激酶 >> PKA
  信号通路 >> 干细胞及 Wnt 通路 >> PKA
  研究领域 >> 神经疾病
• 靶点:

  PKA I

  PKA II

  PDE3A:47.6 μM (Ki)

  PDE10 GAF domain:50 μM (EC50)

• 体外研究: 用Sp-cAMPS(腺苷环3',5'-硫代磷酸酯的刺激性非对映体)治疗肝细胞,模拟胰高血糖素的反应。胰高血糖素刺激的Ca2+水平的增加可以被Sp-camp模仿[4]。
• 体内研究: 在慢性酒精消耗(CAC)小鼠中,直接向前额叶皮质注入Sp-cAMPS(1µg/µL)可显著改善或削弱退缩动物和水动物的工作记忆表现[5]。
• 参考文献:

  [1]. Su H Hung, et al. A new nonhydrolyzable reactive cAMP analog, (Sp)-adenosine-3',5'-cyclic-S-(4-bromo-2,3-dioxobutyl)monophosphorothioate irreversibly inactivates human platelet cGMP-inhibited cAMP phosphodiesterase. Bioorg Chem. 2002 Feb;30(1):16-31.

  [2]. L Y Wang, et al. Regulation of kainate receptors by cAMP-dependent protein kinase and phosphatases. Science. 1991 Sep 6;253(5024):1132-5.

  [3]. Ronald Jäger, et al. Activation of PDE10 and PDE11 phosphodiesterases. J Biol Chem. 2012 Jan 6;287(2):1210-9.

  [4]. P A Connelly,et al. A study of the mechanism of glucagon-induced protein phosphorylation in isolated rat hepatocytes using (Sp)-cAMPS and (Rp)-cAMPS, the stimulatory and inhibitory diastereomers of adenosine cyclic 3',5'-phosphorothioate. J Biol Chem. 1987 Mar 25;262(9):4324-32.

  [5]. G Dominguez, et al. Rescuing prefrontal cAMP-CREB pathway reverses working memory deficits during withdrawal from prolonged alcohol exposure. Brain Struct Funct. 2016 Mar;221(2):865-77.

Sp-cAMPS sodium salt物理化学性质

• 分子式: C₁₀H₁₁N₅NaO₅PS
• 分子量: 367.253
• 精确质量: 367.011627
• PSA: 182.50000
• LogP: 0.96900
• 储存条件: -20°C，密闭，干燥

Sp-cAMPS sodium salt英文别名

• Sodium (2S,4aR,6R,7R,7aS)-6-(6-amino-9H-purin-9-yl)-7-hydroxytetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2-thiolate 2-oxide
• 4H-Furo[3,2-d]-1,3,2-dioxaphosphorin-7-ol, 6-(6-amino-9H-purin-9-yl)tetrahydro-2-mercapto-, 2-oxide, sodium salt, (2S,4aR,6R,7R,7aS)- (1:1)