| 化學(xué)名 | 2( S)-(1( S)-Carboxy-2-(3-(3,5-dichlorobenzyl)-3H-imidazol-4-yl)-ethylamino)-4-methylpentanoic acid |
| 簡(jiǎn)稱 | MLN-4760, ACE2 Inhibitor |
| 別名 | Angiotensin-Converting Enzyme-Related Carboxypeptidase Inhibitor, ML00106791, GL-1001, GL1001, MLN4760 |
| 中文名 | - |
| 化學(xué)式 | C19H23Cl2N3O4 |
| 分子量 | 428.31 |
| CAS號(hào) | 305335-31-3 |
| 純度 | >96% |
| 溶劑/溶解度 | DMSO 10mM, need ultrasonic and warm at 37℃; Water insoluble |
| 溶液配制 | 5mg加入1.167ml DMSO，或者每4.28mg加入1ml DMSO，配制成10mM溶液，超聲并37℃水浴處理。 |
生物信息:
| 產(chǎn)品描述 | MLN-4760 is an effective and selective inhibitor of human ACE2 (IC50, 0.44 nM). It also has excellent selectivity (>5000-fold) versus related enzymes including human testicular ACE (IC50>100 μM) and bovine carboxypeptidase A (CPDA; IC50, 27 μM). MLN-4760 also enables to study the effect of reduced ACE2 activity on the lung’s susceptibility for Coronavirus disease (COVID) related acute respiratory distress syndrome (ARDS). | ||||
| 信號(hào)通路 | Anti COVID-19; Antimicrobial Signaling; Metabolic Enzyme/Protease | ||||
| 靶點(diǎn) | Human ACE2 | Bovine carboxypeptidase A | Human testicular ACE | - | - |
| IC50/EC50 | 0.44 nM | 27 μM | >100 μM | - | - |
| 體外研究 | MLN-4760 is a potent and selective human ACE2 inhibitor (IC50, 0.44 nM), with excellent selectivity (>5000-fold) versus related enzymes human testicular ACE (IC50, >100 μM) and bovine carboxypeptidase A (CPDA; IC50, 27 μM). MLN-4760 effectively quenches cleavage of the 7-Mca-YVADAPK(Dnp) in rhACE2. MLN-4760 shows pIC50 at rhACE2 of 8.5±0.1 and at rhACE of 4.4±0.2. MLN-4760 also shows pIC50 at rhACE2 of 4.7±0.1, 6.9±0.1 and at ACE of 4.4±0.1, 6.2±0.1 in murine heart and mononuclear cells (MNCs), resepctively. | ||||
| 體內(nèi)研究 | MLN-4760 (100 μM, intracerebroventricular infusion for five days) significantly worsens neurological function at 4 h and 3 d post-stroke without significantly increasing infarct volume. | ||||
| 臨床實(shí)驗(yàn) | - | ||||
| 特征 | - | ||||
相關(guān)實(shí)驗(yàn)數(shù)據(jù)(此數(shù)據(jù)來(lái)自于公開(kāi)文獻(xiàn)，并不保證其有效性)：
| 酶活性檢測(cè)實(shí)驗(yàn) | |
| 方法 | N/A |
| 細(xì)胞實(shí)驗(yàn) | |
| 細(xì)胞系 | - |
| 濃度 | - |
| 處理時(shí)間 | - |
| 方法 | - |
| 動(dòng)物實(shí)驗(yàn) | |
| 動(dòng)物模型 | - |
| 配制 | 1. Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline Solubility: ≥ 5 mg/mL (11.67 mM); Clear solution 2. Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in saline) Solubility: ≥ 5 mg/mL (11.67 mM); Clear solution 3. Add each solvent one by one: 10% DMSO 90% corn oil Solubility: ≥ 5 mg/mL (11.67 mM); Clear solution |
| 劑量 | - |
| 給藥方式 | - |
參考文獻(xiàn)：
1. Dales NA, et al. Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors. J Am Chem Soc. 2002 Oct 9;124(40):11852-3.
2. Joshi S, et al. Angiotensin converting enzyme versus angiotensin converting enzyme-2 selectivity of MLN-4760 and DX600 in human and murine bone marrow-derived cells. Eur J Pharmacol. 2016 Mar 5;774:25-33.
3. Bennion DM, et al. Activation of the Neuroprotective Angiotensin-Converting Enzyme 2 in Rat Ischemic Stroke. Hypertension. 2015 Jul;66(1):141-8.
包裝清單：
| 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | 包裝 |
| SF1197-10mM | MLN-4760 (ACE2抑制劑) | 10mM×0.2ml |
| SF1197-5mg | MLN-4760 (ACE2抑制劑) | 5mg |
| SF1197-25mg | MLN-4760 (ACE2抑制劑) | 25mg |
| SF1197-100mg | MLN-4760 (ACE2抑制劑) | 100mg |
| － | 說(shuō)明書 | 1份 |
保存條件：
-20℃保存，至少一年有效。5mg、25mg和100mg包裝也可室溫保存，至少6個(gè)月有效。如果溶于非DMSO溶劑，建議分裝后-80℃保存，預(yù)計(jì)6個(gè)月內(nèi)有效。
注意事項(xiàng)：
本產(chǎn)品僅限于專業(yè)人員的科學(xué)研究用，不得用于臨床診斷或治療，不得用于食品或藥品，不得存放于普通住宅內(nèi)。
為了您的安全和健康，請(qǐng)穿實(shí)驗(yàn)服并戴一次性手套操作。
