Ramiprilat
(Synonyms: 雷米普利,Ramipril Diacid) 目录号 : GC10694
An ACE inhibitor
Cas No.:87269-97-4
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 87269-97-4 | SDF | |
| 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 SMILES | O=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°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.574 mL | 12.87 mL | 25.74 mL |
| 5 mM | 0.5148 mL | 2.574 mL | 5.148 mL |
| 10 mM | 0.2574 mL | 1.287 mL | 2.574 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet