细胞渗透性cAMP类似物,cAMP诱导的PKA激活的竞争性拮抗剂,Rp-cAMPS triethylammonium salt 是 cAMP 的类似物,可作为 cAMP 诱导的依赖 cAMP 的 PKA I 和 PKA II 活化 (Ki 分别为 6.05 µM 和 9.75 µM) 的有效,竞争性和细胞渗透性拮抗剂。Rp-cAMPS triethylammonium salt 耐磷酸二酯酶水解。
生物活性
Rp-cAMPS triethylammonium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 μM and 4.5 μM, respectively) antagonist. Rp-cAMPS triethylammonium salt is resistant to hydrolysis by phosphodiesterases.
性状
Solid
IC50 & Target[1][2]
Ki: 6.05 μM (PKA I) and 9.75 μM (PKA II)
体外研究(In Vitro)
A membrane-permeable competitive cAMP antagonist (Rp-cAMPS) that blocks PKA activation by binding to the regulatory subunits without dissociating the kinase holoenzyme also inhibits synaptic plasticity but has no effect on normal synaptic transmission.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Rp-cAMPS (10 μM, 15 min) decreases the monosynaptic EPSCs evoked at the PB-CeLC and BLA-CeLC synapses in slices from arthritic rats but not in control neurons from normal animals. The inhibitory effect of Rp-cAMPS is significant compared to predrug (ACSF) control values obtained in the same neurons.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.