| Bioactivity | KMUP-4, as a xanthine derivative with cGMP-enhancing activity, induces aortic relaxation through endothelium-dependent and independent mechanisms. KMUP-4 increases cytoplasmic cyclic guanosine monophosphate (cGMP) and cyclic adenosine monophosphate (cAMP) levels by inhibiting phosphodiesterases (PDEs) and activating K+ channels. KMUP-4 can be used in the study of cardiovascular diseases[1]. |
| Invitro | KMUP-4 (1 nM-100 mM) 累积浓度对脱内皮主动脉 (E2) 产生浓度依赖性的血管松弛作用 (pEC50=5.94)，对完整内皮主动脉 (E+) 产生浓度依赖性的血管松弛作用 (pEC50=6.45)，表明 KMUP-4 的血管舒张效应部分依赖于内皮细胞[1]。KMUP-4 (10 mM) 对 PDE3、PDE4 和 PDE5 的抑制活性分别为 56%、33% 和 15%[1]。KMUP-4 (0.1 mM，18 h) 显著增加人脐静脉内皮细胞中 eNOS 蛋白的表达[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> KMUP-4 相关抗体: |
| CAS | 864873-81-4 |
| Formula | C19H23N7O4 |
| Molar Mass | 413.43 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. BN Wu, et al. Aortic Smooth Muscle Relaxants KMUP-3 and KMUP-4, Two Nitrophenylpiperazine Derivatives of Xanthine, Display cGMP-Enhancing Activity: Roles of Endothelium, Phosphodiesterase, and K:+: Channel. Journal of cardiovascular pharmacology 46.5 (2005): 600-608. |