化学名 | 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 |
简称 | DX600 (ACE2 Inhibitor) |
别名 | Ac-GDYSHCSPLRYYPWWKCTYPDPEGGG-NH2 |
中文名 | DX600 (ACE2抑制剂) |
化学式 | C141H187N35O40S2 |
分子量 | 3076.4 |
CAS号 | - |
纯度 | >95% |
溶剂/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。 |
产品描述 | 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. | ||||
信号通路 | Anti COVID-19; Antimicrobial Signaling; Metabolic Enzyme/Protease | ||||
靶点 | Recombinant Human ACE2 | Mouse ACE2 | Rat ACE2 | - | - |
IC50 | 0.1μM | 7μM | 7μM | - | - |
体外研究 | - | ||||
体内研究 | - | ||||
临床实验 | - | ||||
特征 | - |
酶活性检测实验 | |
方法 | N/A |
细胞实验 | |
细胞系 | human mononuclear cells, human CD34+ cells, mouse mononuclear cells (MNCs), murine lineage-depleted cells |
浓度 | 10-12M, 10-10M, 10-8M, 10-6M, 10-4M, 10-2M |
处理时间 | - |
方法 | - |
动物实验 | |
动物模型 | - |
配制 | - |
剂量 | - |
给药方式 | - |
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.
包装清单:产品编号 | 产品名称 | 包装 |
SF1201-5mg | DX600 (ACE2抑制剂) | 5mg |
SF1201-25mg | DX600 (ACE2抑制剂) | 25mg |
SF1201-100mg | DX600 (ACE2抑制剂) | 100mg |
- | 说明书 | 1份 |
-20℃保存,至少一年有效。如果溶于非DMSO溶剂,建议分装后-80℃保存,预计6个月内有效。
注意事项:本产品仅限于专业人员的科学研究用,不得用于临床诊断或治疗,不得用于食品或药品,不得存放于普通住宅内。
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