Enalaprilat Dihydrate

別名:MK-422 Dihydrate

Enalaprilat (MK-422) is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 1.94 nM.

Enalaprilat Dihydrate化学構造

CAS No. 84680-54-6

サイズ 価格(税別) 在庫状況
JPY 20200 国内在庫あり
JPY 101400 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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Enalaprilat Dihydrate関連製品

シグナル伝達経路

RAAS阻害剤の選択性比較

生物活性

製品説明 Enalaprilat (MK-422) is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 1.94 nM.
特性 The 1st dicarboxylate-containing ACE inhibitor developed to overcome captopril limitations.
Targets
ACE [1]
1.94 nM
In Vitro
In vitro Enalaprilat has high affinity for human endothelial ACE with IC50 of 1.94 nM in vitro binding assay by displacing a saturating concentration of [125I]351A, a radiolabeled lisinopril analogue from ACE binding sites, and shows bradykinin/angiotensin I selectivity ratio of 1.00 calculated from double displacement experiments. [1] Enalaprilat has the strong inhibitory effect on Aβ42-to-Aβ40-converting activity found in the N-domain of ACE, exhibiting a 10-fold lower IC50 (0.003~0.01 μM) than captopril (0.03~0.1 μM). [2] Enalaprilat (100 nM) blocks protein kinase C epsilon by directly activating bradykinin B1 receptor at the canonical Zn2+ binding site, leading to prolonged nitric oxide (NO) production in cytokine-treated human lung microvascular endothelial cells. [3] Enalaprilat attenuates the IGF-I induced neonatal rat cardiac fibroblast growth (30% reduction) in a concentration-dependent fashion, with IC50 of 90 mM. [4]
Kinase Assay Single displacement binding assay
The binding assay is based on the competitive displacement of [125I]351A by Enalaprilat performed on whole endothelial cells. Subconfluent HUVECs in 6-well plates are rinsed with 2 mL binding buffer (140 mM NaCl, 2.7 mM KCl, 1.8 mM CaCl2, 1.03 mM MgCl2, 0.42 mM NaH2PO4, 10 mM HEPES, 2 mM sodium pyruvate and 5 mM glucose, pH 7.4), and the culture medium is replaced with 2.5 mL fresh binding buffer containing 5% fetal bovine serum (FBS). The Enalaprilat (2.5-12.5 μL, 0.1-50 nM) or equivalent volumes of diluent are added to the binding buffer. A saturating amount of [125I]351A (10 μL, typically 106 cpm) is then added to each sample and the plates are incubated at 37 °C for 2 hours in a thermostatic bath. The cells are then rinsed twice with 1.5 mL binding buffer. Finally, the cells are extracted with 0.5 mL NaOH 1 N, incubated for 5 minutes, and the radioactivity is counted with a gamma counter. The ratio of specific [125I]351A bound to total bound activity (B/B0) is calculated, and the inhibitory potency of Enalaprilat expressed as the concentration of ACE inhibitors able to displace 50% of the bound radioligand, i.e. the IC50.
細胞実験 細胞株 Rat cardiac fibroblasts cell lines
濃度 Dissolved in DMSO, final concentrations 1 nM - 10 μM
反応時間 24 hours
実験の流れ After 24 hours incubation in serum-free medium (DMEM), cells are stimulated with IGF-I (1-100 nM) and coincubated with Enalaprilat (1 nM-10 μM) for 24 hours. Cellular proliferation is assessed by 5-bromo-2'-deoxyuridine (BrdU) incorporation during the last 4 hours of the 24 hours incubation period using a colorimetric immunoassay. The extinctions are measured at 450 nm in an ELISA plate reader. All values consist of an n=9.
In Vivo
In Vivo Enalaprilat has unfavourable ionisation characteristics to allow sufficient potency for oral administration, thus Enalaprilat is only suitable for intravenous administration, which is overcome by the esterification with ethanol to produce Enalapril. Administration of Enalaprilat induces a significant reduction of MAP at 70 minutes compared with the placebo group during haemorrhagic shock in rats, and results in a 50% reduction of CO, a general tendency of EB extravasation which is significant in the kidney and lungs, and a significant increase in ileal EB extravasation (53%). [5] Enalaprilat has no effect in nonhypertrophied hearts, but significantly attenuates the greater increase in left ventricular end-diastolic pressure in hypertrophied hearts compared with no drug. [6]
動物実験 動物モデル Male Sprague–Dawley rats
投与量 1 mg/kg
投与経路 I.V. bolus
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03051282 Active not recruiting
Healthy Volunteers
University of Michigan
April 1 2017 Phase 4
NCT02654678 Unknown status
Heart Failure|Dilated Cardiomyopathy|Congenital Heart Disease
Ethicare GmbH
March 2016 Phase 2|Phase 3
NCT02652728 Unknown status
Heart Failure|Dilated Cardiomyopathy
Ethicare GmbH
January 2016 Phase 2|Phase 3
NCT02652741 Unknown status
Heart Failure|Congenital Heart Disease
Ethicare GmbH
January 2016 Phase 2|Phase 3

化学情報

分子量 348.4 化学式

C18H24N2O5.2H2O

CAS No. 84680-54-6 SDF Download Enalaprilat Dihydrate SDFをダウンロードする
Smiles CC(C(=O)N1CCCC1C(=O)O)NC(CCC2=CC=CC=C2)C(=O)O.O.O
保管

In vitro
Batch:

DMSO : 70 mg/mL ( (200.91 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 5 mg/mL

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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