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Ramipril

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Chemical Structure| 87333-19-5 同义名 : HOE-498
CAS号 : 87333-19-5
货号 : A271148
分子式 : C23H32N2O5
纯度 : 98%
分子量 : 416.511
MDL号 : MFCD00865775
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(252.09 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 1 mg/mL(2.4 mM)，配合低频超声助溶
动物实验配方：

30% PEG400+0.5% Tween80+5% propylene glycol+water 30 mg/mL suspension

生物活性
靶点

  • ACE

    ACE, IC50:5 nM
描述 Ramipril is a angiotensin converting enzyme (ACE) inhibitor. Ramipril benefited left ventricular remodeling by reducing fibrosis and collagen accumulation in the left ventricle of rats after myocardial infarction[3]. Ramipril inhibits systolic blood pressure (SBP) with IC50 of 1.97 mg/kg in spontaneously hypertensive rats (SHR). Cardiac ACE activity was greatly reduced by ramipril independently of SBP reduction and dosage[4]. Prolonged ramiprilat treatment increased ACE expression in primary cultures of human endothelial cells and in vivo (mouse lung) [5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00732069 End Stage Renal Failure on Dia... 展开 >>lysis Complication of Hemodialysis 收起 << Phase 2 Completed - United States, Tennessee ... 展开 >> Vanderbilt University Medical Center Nashville, Tennessee, United States, 37323 收起 <<
NCT00732069 - Completed - -
NCT01225445 Biopsy-confirmed IgA Nephropat... 展开 >>hy Proteinuria Less Than 0.5 g Per Day Normal Blood Pressure Serum Creatinine Below 120 Umol/l 收起 << Phase 3 Completed - Hong Kong ... 展开 >> Department of Medicine & Therapeutics, Prince of Wales Hospital Shatin, Hong Kong 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

12.00mL

2.40mL

1.20mL

24.01mL

4.80mL

2.40mL
参考文献

[1]Kohlstedt K, Brandes RP, et al. Angiotensin-converting enzyme is involved in outside-in signaling in endothelial cells. Circ Res. 2004 Jan 9;94(1):60-7. Epub 2003 Nov 13.

[2]Stevens BR, Phillips MI, et al. Ramipril inhibition of rabbit (Oryctolagus cuniculus) small intestinal brush border membrane angiotensin converting enzyme. Comp Biochem Physiol C. 1988;91(2):493-7.

[3]Wei Q, Liu H, Liu M, Yang C, Yang J, Liu Z, Yang P. Ramipril attenuates left ventricular remodeling by regulating the expression of activin A-follistatin in a rat model of heart failure. Sci Rep. 2016 Sep 19;6:33677. doi: 10.1038/srep33677. PMID: 27642098; PMCID: PMC5027547.

[4]Raasch W, Jöhren O, Schwartz S, Gieselberg A, Dominiak P. Combined blockade of AT1-receptors and ACE synergistically potentiates antihypertensive effects in SHR. J Hypertens. 2004 Mar;22(3):611-8. doi: 10.1097/00004872-200403000-00025. PMID: 15076168.

[5]Kohlstedt K, Brandes RP, Müller-Esterl W, Busse R, Fleming I. Angiotensin-converting enzyme is involved in outside-in signaling in endothelial cells. Circ Res. 2004 Jan 9;94(1):60-7. doi: 10.1161/01.RES.0000107195.13573.E4. Epub 2003 Nov 13. PMID: 14615289.