公告提醒:爱必信所有产品和服务仅用于科学研究,不用于临床应用及其他用途提供产品和服务(也不为任何个人提供产品和服务)! 抑制剂描述: 产品名称:Ramipril 产品别名:见爱必信官网 英文别名:Ramipril 靶点:ACE CAS:87333-19-5 纯度:>98% 外观:见爱必信官网 保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. 描述: Ramipril 是血管紧张素转换酶(ACE)抑制剂,IC50为5 nM。Ramipril作用于培养的内皮细胞,增强ACE结合的CK2的活性,及 ACE在Ser1270位点磷酸化,但是作用于表达S1270A ACE 突变或ACE缺陷的细胞,不能激活JNK或不能刺激c-Jun在核内累积。长期使用Ramipril治疗原代培养的人类内皮细胞,提高ACE表达, 这种作用可被JNK抑制剂SP600125阻断。 Ramipril 作用于血清饥饿法处理的体外内皮细胞,对凋亡率没有增强效果。 溶解性:Ethanol :41.7 mg/mL (100 mM) DMSO :41.7 mg/mL (100 mM) 体外研究: Ramipril is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 5 nM. Ramipril enhances the activity of ACE-associated CK2 and the phosphorylation of ACE Ser1270 in cultured endothelial cells, but is unable to activate JNK or stimulate the nuclear accumulation of c-Jun in endothelial cells expressing a S1270A ACE mutant or in ACE-deficient cells. Prolonged Ramipril treatment increases ACE expression in primary cultures of human endothelial cells and in vivo (mouse lung), which can be prevented by pretreatment with the JNK inhibitor SP600125. Ramipril displays little enhanced effect on the rate of in vitro endothelial apoptosis induced by the serum deprivation method. 体内研究:Chronic in vivo administration of Ramipril to rats at a dosage that has similar hypotensive effects in vitro HUVECs significantly reduces the rate of LPS-induced apoptosis compared to the other ACE inhibitors, which contrasts with the apoptosis effect in vitro. Ramipril inhibits systolic blood pressure (SBP) with IC50 of 1.97 mg/kg in spontaneously hypertensive rats (SHR). When in combination with AT1-receptor blockade by candesartan-cilexetil increases SBP reduction synergistically rather than additively. Administration of Ramipril to spontaneously hypertensive rats (SHR) produces significant inhibition of aorta ACE and lung ACE with IC50 ~5 mg/kg, but shows little effect for brain ACE ex vivo. Ramipril prevents beta cell dysfunction in osteoprotegerin treated mice through decreasing islet monocyte/macrophage infiltration, fibrosis and apoptosis involving decreasing RAS, growth factor genes and inflammatory molecules expressions. 产品信息订购:
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