| 化學(xué)名 | Ac-Gly-Asp-Tyr-Ser-His-Cys-Ser-Pro-Leu-Arg-Tyr-Tyr-Pro-Trp-Trp-Lys-Cys-Thr-Tyr-Pro-Asp-Pro-Glu-Gly-Gly-Gly-NH2 |
| 簡(jiǎn)稱 | DX600 (ACE2 Inhibitor) |
| 別名 | Ac-GDYSHCSPLRYYPWWKCTYPDPEGGG-NH2 |
| 中文名 | DX600 (ACE2抑制劑) |
| 化學(xué)式 | C141H187N35O40S2 |
| 分子量 | 3076.4 |
| CAS號(hào) | - |
| 純度 | >95% |
| 溶劑/溶解度 | H2O: 78mg/ml (25mM); DMSO: 30mg/ml |
| 溶液配制 | 5mg加入160μl ddH2O，或者每31.25mg加入1ml ddH2O，配制成10mM溶液。 |
生物信息:
| 產(chǎn)品描述 | DX600 is a potent and selective peptide inhibitor of angiotensin-converting enzyme 2 (ACE2; Kis = 2.8, 200, and 1,200 nM for recombinant, human, and murine ACE2, respectively). ACE2 is an enzyme that is cardioprotective and renoprotective. Inhibition of ACE2 with DX600 reduces in vitro vascular repair by CD34+ stem/progenitor cells and exacerbates myocardial injury and dysfunction in vivo. DX600 is a 26-amino acid peptide and contains two free cysteine residues and tends to polymerize. Polymerization and oxidation of DX600 might conceivably affect binding to and inhibition of ACE2, so it is recommends dissolving DX600 just before use. | ||||
| 信號(hào)通路 | Anti COVID-19; Antimicrobial Signaling; Metabolic Enzyme/Protease | ||||
| 靶點(diǎn) | Recombinant Human ACE2 | Mouse ACE2 | Rat ACE2 | - | - |
| IC50 | 0.1μM | 7μM | 7μM | - | - |
| 體外研究 | - | ||||
| 體內(nèi)研究 | - | ||||
| 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 | human mononuclear cells, human CD34+ cells, mouse mononuclear cells (MNCs), murine lineage-depleted cells |
| 濃度 | 10-12M, 10-10M, 10-8M, 10-6M, 10-4M, 10-2M |
| 處理時(shí)間 | - |
| 方法 | - |
| 動(dòng)物實(shí)驗(yàn) | |
| 動(dòng)物模型 | - |
| 配制 | - |
| 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.
4.Kim Brint Pedersen, et al. Species-specific inhibitor sensitivity of angiotensin-converting enzyme 2(ACE2) and its implication for ACE2 activity assays. Am J Physiol Regul Integr Comp Physiol. 2011, 301: R1293–R1299.
包裝清單：
| 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | 包裝 |
| SF1201-5mg | DX600 (ACE2抑制劑) | 5mg |
| SF1201-25mg | DX600 (ACE2抑制劑) | 25mg |
| SF1201-100mg | DX600 (ACE2抑制劑) | 100mg |
| － | 說(shuō)明書(shū) | 1份 |
保存條件：
-20℃保存，至少一年有效。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。
