Enalapril (MK-421)
(Synonyms: 依那普利; MK-421) 目录号 : GC32499
依那普利 (MK-421) (MK-421) 是一种血管紧张素转换酶 (ACE) 抑制剂，可用于高血压疾病的研究。
Cas No.:75847-73-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Enalapril (MK-421) is an angiotensin converting enzyme (ACE) inhibitor.
Enalapril (MK-421) belongs to a class of medications called angiotensin converting enzyme inhibitors. Normally angiotensin I is converted to angiotensin II by angiotensin converting enzyme (ACE). Angiotensin II constricts blood vessels, increasing blood pressure. By inhibiting ACE, Enalapril (MK-421) decreases levels of angiotensin II leading to less vasoconstriction and decreased blood pressure[1].
[1]. http://en.wikipedia.org/wiki/Enalapril
| Cas No. | 75847-73-3 | SDF | |
| 别名 | 依那普利; MK-421 | ||
| Canonical SMILES | O=C(O)[C@H]1N(C([C@H](C)N[C@H](C(OCC)=O)CCC2=CC=CC=C2)=O)CCC1 | ||
| 分子式 | C20H28N2O5 | 分子量 | 376.45 |
| 溶解度 | Soluble in DMSO | 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 | 2.6564 mL | 13.282 mL | 26.564 mL |
| 5 mM | 0.5313 mL | 2.6564 mL | 5.3128 mL |
| 10 mM | 0.2656 mL | 1.3282 mL | 2.6564 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。
Effects of Enalapril on mortality in severe congestive heart failure. Results of the Cooperative North Scandinavian Enalapril Survival Study (CONSENSUS)
N Engl J Med 1987 Jun 4;316(23):1429-35.PMID:2883575DOI:10.1056/NEJM198706043162301.
To evaluate the influence of the angiotensin-converting-enzyme inhibitor Enalapril (2.5 to 40 mg per day) on the prognosis of severe congestive heart failure (New York Heart Association [NYHA] functional class IV), we randomly assigned 253 patients in a double-blind study to receive either placebo (n = 126) or Enalapril (n = 127). Conventional treatment for heart failure, including the use of other vasodilators, was continued in both groups. Follow-up averaged 188 days (range, 1 day to 20 months). The crude mortality at the end of six months (primary end point) was 26 percent in the Enalapril group and 44 percent in the placebo group--a reduction of 40 percent (P = 0.002). Mortality was reduced by 31 percent at one year (P = 0.001). By the end of the study, there had been 68 deaths in the placebo group and 50 in the Enalapril group--a reduction of 27 percent (P = 0.003). The entire reduction in total mortality was found to be among patients with progressive heart failure (a reduction of 50 percent), whereas no difference was seen in the incidence of sudden cardiac death. A significant improvement in NYHA classification was observed in the Enalapril group, together with a reduction in heart size and a reduced requirement for other medication for heart failure. The overall withdrawal rate was similar in both groups, but hypotension requiring withdrawal occurred in seven patients in the Enalapril group and in no patients in the placebo group. After the initial dose of Enalapril was reduced to 2.5 mg daily in high-risk patients, this side effect was less frequent. We conclude that the addition of Enalapril to conventional therapy in patients with severe congestive heart failure can reduce mortality and improve symptoms. The beneficial effect on mortality is due to a reduction in death from the progression of heart failure.
Enalapril maleate (MK-421), a potent, nonsulfhydryl angiotensin-converting enzyme inhibitor: absorption, disposition, and metabolism in man
Drug Metab Rev 1983;14(1):99-110.PMID:6301792DOI:10.3109/03602538308991383.
Animal studies (particularly in dogs) on Enalapril maleate have served to predict the patterns of absorption and elimination observed in man. Enalapril is more readily absorbed in man than the active inhibitor form MK-422. Estimates of minimum absorption of Enalapril are of the order of 60-70%, based on urinary recovery. Metabolism of Enalapril to MK-422 appears to be largely a postabsorptive process. From urinary recovery data, a minimum of 43% of a 10-mg dose of Enalapril is available as MK-422. Excretion of Enalapril and MK-422 is principally renal. The excellent mass balance obtained in human studies precludes extensive metabolism beyond hydrolysis to MK-422. Data in hand suggest that any metabolism other than to MK-422 is of a trace nature.
Enalapril: a review of human pharmacology
Drugs 1985;30 Suppl 1:13-24.PMID:2994984DOI:10.2165/00003495-198500301-00004.
Enalapril, an orally-active, long-acting, nonsulphydryl angiotensin-converting enzyme (ACE) inhibitor, is extensively hydrolysed in vivo to enalaprilat, its bioactive form. Bioactivation probably occurs in the liver. Metabolism beyond activation to enalaprilat is not observed in man. Administration with food does not affect the bioavailability of Enalapril; excretion of Enalapril and enalaprilat is primarily renal. Peak serum enalaprilat concentrations are reached 4 hours post-dose, and the profile is polyphasic with a prolonged terminal half-life (greater than 30 hours) due to the binding of enalaprilat to ACE. Steady-state is achieved by the fourth daily dose, with no evidence of accumulation. The effective accumulation half-life following multiple dosing is 11 hours. Higher serum concentrations and delayed urinary excretion occur in patients with severe renal insufficiency. Enalapril reduces blood pressure in hypertensive patients by decreasing systemic vascular resistance. The blood pressure reduction is not accompanied by an increase in heart rate. Furthermore, cardiac output is slightly increased and cardiovascular reflexes are not impaired. Once- and twice-daily dosage regimens reduce blood pressure to a similar extent. Enalapril increases renal blood flow and decreases renal vascular resistance. Enalapril also augments the glomerular filtration rate in patients with a glomerular filtration rate less than 80 ml/min. Enalapril reduces left ventricular mass, and does not affect cardiac function or myocardial perfusion during exercise. There is no rebound hypertension after Enalapril therapy is stopped. Enalapril does not produce hypokalaemia, hyperglycaemia, hyperuricaemia or hypercholesterolaemia. When combined with hydrochlorothiazide, Enalapril attenuates the undesirable diuretic-induced metabolic changes. Therapeutic doses of Enalapril do not affect serum prolactin and plasma cortisol in healthy volunteers or T3, rT3, T4 and TSH in hypertensive patients. Enalapril has natriuretic and uricosuric properties. The antihypertensive effect of Enalapril is potentiated by hydrochlorothiazide, timolol and methyldopa, but unaffected by indomethacin and sulindac. No interactions occur between Enalapril and frusemide, hydrochlorothiazide, digoxin and warfarin. The bioavailability of Enalapril is slightly reduced when propranolol is coadministered, but this does not appear to be of any clinical significance. Enalapril increases cardiac output and stroke volume and decreases pulmonary capillary wedge pressure in patients with congestive heart failure refractory to conventional treatment with digitalis and diuretics.(ABSTRACT TRUNCATED AT 400 WORDS)
Antihypertensive treatment with calcium channel blockers and renal protection: focus on lercanidipine and lercanidipine/Enalapril
Eur Rev Med Pharmacol Sci 2022 Oct;26(20):7482-7492.PMID:36314318DOI:10.26355/eurrev_202210_30018.
Objective: The aim of the study was to review the literature on clinical pharmacology of lercanidipine and experimental and clinical evidence and evaluate its ability to reduce proteinuria and preserve renal function when used as monotherapy or in combination with the angiotensin-converting enzyme (ACE) inhibitor Enalapril. Materials and methods: MEDLINE/PubMed was searched for appropriate keywords. Results: Lercanidipine, a third-generation calcium channel blocker, has been shown to have a unique pharmacological and clinical profile, which translates into favorable renal hemodynamic changes. The fixed-dose combination lercanidipine/Enalapril has been proposed to overcome unmet therapeutic needs, often as the initial treatment in the high-risk patient. Conclusions: Lercanidipine may be regarded as an ideal antihypertensive drug for patients at renal risk and possibly the preferred choice among calcium channel blocker drugs.
Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Enalapril
J Pharm Sci 2017 Aug;106(8):1933-1943.PMID:28435140DOI:10.1016/j.xphs.2017.04.019.
Literature data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the marketing authorization of immediate-release, solid oral dosage forms containing Enalapril maleate are reviewed. Enalapril, a prodrug, is hydrolyzed by carboxylesterases to the active angiotensin-converting enzyme inhibitor enalaprilat. Enalapril as the maleate salt is shown to be highly soluble, but only 60%-70% of an orally administered dose of Enalapril is absorbed from the gastrointestinal tract into the enterocytes. Consequently, Enalapril maleate is a Biopharmaceutics Classification System class III substance. Because in situ conversion of the maleate salt to the sodium salt is sometimes used in production of the finished drug product, not every Enalapril maleate-labeled finished product actually contains the maleate salt. Enalapril is not considered to have a narrow therapeutic index. With this background, a biowaiver-based approval procedure for new generic products or after major revisions to existing products is deemed acceptable, provided the in vitro dissolution of both test and reference preparation is very rapid (at least 85% within 15 min at pH 1.2, 4.5, and 6.8). Additionally, the test and reference product must contain the identical active drug ingredient.