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| 中文名称： | E 64c | 中文别名： | E 64c |
|---|---|---|---|
| 英文名称： | E 64c | CAS： | 76684-89-4 |
| 产品分类： | 小分子化合物 | 纯度： | ≥98% |
| 产品编号 | 品牌 | 纯度 | 规格 | 库存 | 价格 |
|---|---|---|---|---|---|
| IE2270 | 索莱宝 | ≥98% | 1mg | 有现货 | 590.00 元 |
| IE2270 | 索莱宝 | ≥98% | 5mg | 有现货 | 1,290.00 元 |
| IE2270 | 索莱宝 | ≥98% | 10mg | 有现货 | 2,190.00 元 |
| 标准名称: | 阿洛司他丁酸 | 英文名称： | E 64c |
|---|---|---|---|
| CAS： | 76684-89-4 | 分子式： | C15H26N2O5 |
| 分子量： | 314.377344608307 | 颜色与性状： | |
| 密度： | 沸点： | ||
| 熔点： | 水溶性： |
| CAS | 76684-89-4 |
| 英文名称 | E 64c |
| 分子式 | C15H26N2O5 |
| 分子量 | 314.38 |
| 规格 | 1mg ; 5mg ; 10mg |
| 溶解性 | Soluble in DMSO ≥25mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 | 冷藏运输 |
| MDL | MFCD00132882 |
| InChIKey | SCMSYZJDIQPSDI-SRVKXCTJSA-N |
| 靶点 | cysteine protease;Calcium-activated neutral protease (CANP);cathepsin C |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | E 64c是一种不可逆的膜渗透性cysteine protease抑制剂，也是Calcium-activated neutral protease (CANP)的抑制剂和cathepsin C的弱不可逆抑制剂。 |
| 生物活性 | E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases， a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.[1-4] |
| In Vitro | E-64c， a derivative of naturally occurring epoxide inhibitor of cysteine proteases， with papain; especially with regard to the hydrogen bonding and hydrophobic interactions of the ligands with conserved residues in the catalytic binding site[1]. E 64c (k2/Ki=140±5M-1s-1) is demonstrated to be a lead structure for the development of irreversible cathepsin C inhibitors[3]. |
| In Vivo | The t-1/2 of plasma E-64c is 0.48 hours. The hemodynamic effects of E-64c are absent at this dose. Using two way analysis of variance， the effects of reperfusion (p=0.0016) or E-64c (p=0.0226) per se on infarct size are significant. In comparing Group A with Group B and Group C with Group D， the depletion of CPK in the E-64c treated groups (Groups A and C) is slightly less than in the vehicle-injected groups (Groups B and D). The insufficient effect of E-64c alone may be explained by the early administration and relatively short t-1/2. Since the effectiveness of NCO-700 has been established，6)，7) our findings might indicate a small but beneficial effect of E-64c on infarct size and CPK content[2]. |
| 动物实验 | Dogs[2]Studies are carried out in 83 mongrel dogs with a mean weight of 11.2kg. They are anesthetized with intravenous sodium thiamylal (7mg/kg). An intravenous bolus of E-64c (100mg/kg)， dissolved in saturated sodium bicarbonate， is administered immediately before the occlusion and after reperfusion in Group A (n=17)， whereas Group B (n=17) receive only the vehicle solution at these times. In the remaining 49 dogs (Groups C and D)， the LAD is permanently ligated at the same level and an intravenous bolus of either Loxistatin acid (100mg/kg) (Group C; n=24) or vehicle only (Group D; n=25) is given immediately before and 1 hour after the ligation. The dose of E-64c is designed for its possible use in clinical practice and the estimated intramyocardial Loxistatin acid molecular concentration is 1，000 times that of total mCANP[2]. |
| 数据来源文献 | [1]. Khan MS， et al. Design， synthesis， evaluation and thermodynamics of 1-substituted pyridylimidazo[1，5-a]pyridine derivatives as cysteine protease inhibitors. PLoS One. 2013 Aug 5;8(8):e69982. [2]. Toda G， et al. Calcium-activated neutral protease inhibitor (E-64c) and reperfusion for experimental myocardial infarction. Jpn Heart J. 1989 May;30(3):375-86. [3]. Radzey H， et al. E-64c-hydrazide: a lead structure for the development of irreversible cathepsin C inhibitors. ChemMedChem. 2013 Aug;8(8):1314-21. [4]. Ji Yeun Kim， et al. Safe， High-Throughput Screening of Natural Compounds of MERS-CoV Entry Inhibitors Using a Pseudovirus Expressing MERS-CoV Spike Protein. Int J Antimicrob Agents. 2018 Nov;52(5):730-732. |
| 单位 | 瓶 |
| 1mM-5mg | 15.9043mL |
| 1mM-1mg | 3.1809mL |
| 1mM-10mg | 31.8086mL |
| 5mM-1mg | 0.6362mL |
| 5mM-5mg | 3.1809mL |
| 5mM-10mg | 6.3617mL |
| 10mM-1mg | 0.3181mL |
| 10mM-5mg | 1.5904mL |
| 10mM-10mg | 3.1809mL |
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| 纯度 | 品牌 | 规格 | 发货地 |
|---|---|---|---|
| - | 索莱宝 | 20mg | 北京 |
