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Alacepril

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Chemical Structure| 74258-86-9 同义名 : DU-1219;Cetapril;Alaceprilum
CAS号 : 74258-86-9
货号 : A465222
分子式 : C20H26N2O5S
纯度 : 95%
分子量 : 406.496
MDL号 : MFCD00869538
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(258.31 mM)，配合低频超声助溶，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
动物实验配方：
生物活性
描述 Alacepril is a relatively novel angiotensin-converting enzyme inhibitor. Alacepril as treatment for MVD (mitral valve disease) is well tolerated in most dogs, and different conditions of cardiac loading may influence the effect of the drug. Alacepril is expected to improve the quality of life of dogs with early stage MVD[3]. Approximately 0.6-0.7 mM of alacepril inhibited 50% of the ROS production by BAL cells from COPD (chronic obstructive pulmonary disease) patients, whereas a slightly higher concentration (3 mM) of lisinopril, an ACE inhibitor not bearing an SH-group, was necessary to inhibit the production of ROS(reactive oxygen species)[4]. Alacepril significantly suppresses the augmented cardiovascular and sympathetic nervous responses to mental stress in patients with essential hypertension[5]. Alacepril was effective in essential hypertension both at rest and during exercise, suggesting that the antihypertensive effect during exercise might be related to the decrease in pressor hormones, especially in plasma angiotensin II[6]. Alacepril prevents the development of atherosclerosis by reducing vascular ACE (angiotensin-converting enzyme) activity in monkeys given a high-cholesterol diet[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.30mL

2.46mL

1.23mL

24.60mL

4.92mL

2.46mL
参考文献

[1]Sakatani A, Miyagawa Y, et al. Evaluation of the effect of an angiotensin-converting enzyme inhibitor, alacepril, on drug-induced renin-angiotensin-aldosterone system activation in normal dogs. J Vet Cardiol. 2016 Sep;18(3):248-54.

[2]Nonoguchi H, Kiyama S, et al. Long-term plasma levels and dose modulation of alacepril in patients with chronic renal failure. Hypertens Res. 2008 Jan;31(1):29-36.

[3]Hori Y, Nakamura K, Kanno N, Hitomi M, Yamashita Y, Hosaka S, Isayama N, Mimura T. Effects of the angiotensin-converting enzyme inhibitor alacepril in dogs with mitral valve disease. J Vet Med Sci. 2018 Aug 10;80(8):1212-1218

[4]Teramoto S, Suzuki M, Matsuse T, Ishii T, Fukuchi Y, Ouchi Y. Effects of angiotensin-converting enzyme inhibitors on spontaneous or stimulated generation of reactive oxygen species by bronchoalveolar lavage cells harvested from patients with or without chronic obstructive pulmonary disease. Jpn J Pharmacol. 2000 May;83(1):56-62

[5]Saitoh M, Miyakoda H, Kitamura H, Kinugawa T, Kotake H, Mashiba H. Effects of an angiotensin-converting enzyme inhibitor, alacepril, on cardiovascular and sympathetic nervous responses to mental stress in patients with essential hypertension. Intern Med. 1993 Sep;32(9):691-4

[6]Kinugawa T, Kitamura H, Ogino K, Noguchi N, Matsumoto T, Hisatome I, Miyakoda H, Kotake H, Mashiba H. Effect of alacepril on blood pressure and neurohumoral factors at rest and during dynamic exercise in patients with essential hypertension. Br J Clin Pharmacol. 1992 Oct;34(4):366-9

[7]Miyazaki M, Takai S. Antiatherosclerotic effect of alacepril, an angiotensin-converting enzyme inhibitor, in monkeys fed a high-cholesterol diet. Hypertens Res. 1999 Mar;22(1):49-54