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Ramiprilat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ramiprilat图片
CAS NO:87269-97-4
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
Ramipril (HOE 498 diacid) 是 Ramipril 的活性代谢物,是一种有效的、具有口服活性的血管紧张素转换酶 (ACE) 抑制剂,Ki 值为 7 pM。
Cas No.87269-97-4
别名雷米普利,Ramipril Diacid
化学名(2S,3aS,6aS)-1-[(2S)-2-[[(1S)-1-carboxy-3-phenylpropyl]amino]-1-oxopropyl]octahydro-cyclopenta[b]pyrrole-2-carboxylic acid
Canonical SMILESO=C([C@H](C)N[C@H](C(O)=O)CCC1=CC=CC=C1)N2[C@]3([H])[C@](CCC3)([H])C[C@H]2C(O)=O
分子式C21H28N2O5
分子量388.5
溶解度≤1mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

pKi= 9.08 in human heart

Ramiprilat is an angiotensin-converting enzyme (ACE) inhibitor.

ACE inhibitors help relax blood vessels and prevent an enzyme from producing angiotensin II, a substance narrowing blood vessels and releasing hormones that can raise blood pressure.

In vitro: Pretreatment with ramiprilat could significantly attenuate the recovery of B2 kinin receptors in while increasing that from membranes lacking caveolin, and such effect was not because of the inhibition of bradykinin degradation. Ramiprilat could also decrease [3H]bradykinin binding to CR membranes. In addition, ramiprilat treatment led to reactivation of the B2 receptor in bradykinin-stimulated cells [1].

In vivo: In previous animal study, when compared with the control rats, diabetic rats showed decreased creatinine clearance rate, increased urinary protein excretion and blood pressure, as well as development of tubulointerstitial fibrosis, glomerulosclerosis, and inflammatory cell infiltration. Furthermore, the blocking angiotensin II with ramipril (the prodrug of ramiprilat) was able to significantly improve all of these parameters [2].

Clinical trial: Previous study showed that ramipril at 10 mg/day could significantly reduce the incidence of MI, stroke or death from cardiovascular causes in patients who were at increased risk for the development of ischaemic cardiovascular events [3].

References:
[1] T.  Benzing, I. Fleming, A. Blaukat, et al. Angiotensin-converting enzyme inhibitor ramiprilat interferes with the sequestration of the B2 kinin receptor within the plasma membrane of native endothelial cells. Circulation 99(15), 2034-2040 (1999).
[2] Li C, Yang CW, Park CW, Ahn HJ, Kim WY, Yoon KH, Suh SH, Lim SW, Cha JH, Kim YS, Kim J, Chang YS, Bang BK.  Long-term treatment with ramipril attenuates renal osteopontin expression in diabetic rats. Kidney Int. 2003 Feb;63(2):454-63.
[3] Warner GT, Perry CM.  Ramipril: a review of its use in the prevention of cardiovascular outcomes. Drugs. 2002;62(9):1381-405.