E-64.|66701-25-5|(Proteinase inhibitor E 64)-陌孚医药/Medlife

您当前的位置：

E-64. (Synonyms: Proteinase inhibitor E 64)

目录号: PC15612 纯度: ≥98%

CAS No. :66701-25-5

商品编号	规格	价格	会员价
PC15612-5mg	5mg	¥490.00	请登录
PC15612-25mg	25mg	¥1372.00	请登录
PC15612-100mg	100mg	¥4116.00	请登录
PC15612-250mg	250mg	¥9604.00	请登录
PC15612-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥539.00	请登录

Medlife所售产品仅用于科学研究（非临床研究），非药品不可食用，不可用于人体或动物的临床诊断和治疗，我们不为个人提供产品及服务。产品COA等资料，可至下方“质量控制”中下载。

加入购物车在线咨询收藏产品大包装询价

中文名称

E-64.

中文别名

N-(反式-环氧丁二酰基)-L-亮氨酸-4-胍基丁基酰胺;E-64 蛋白酶抑制剂,E-64 Protease Inhibitor;E-64 抑制剂;E-64,蛋白酶抑制剂;L-(反式-环氧丁二酰基)-L-亮氨酸-4-胍基丁基酰胺;反-环氧丁二酰基-L-亮氨酰胺基(4-胍基)丁烷

英文名称

E-64

英文别名

E-64;trans-Epoxysuccinyl-L-leucylamido(4-guanidino)butane;N-(trans-Epoxysuccinyl)-L-leucine 4-guanidinobutylamide;(2S,3S)-3-(((S)-1-((4-Guanidinobutyl)amino)-4-methyl-1-oxopentan-2-yl)carbamoyl)oxirane-2-carboxylic acid;(L-3-TRANS-CARBOXYOXIRANE-2-CARBONYL)-L-LEUCYLAGMATINE HEMIHYDRATE;E 64;L-trans-Epoxysuccinyl-Leu-4-guanidinobutylamide;TRANS-EPOXYSUCCINYL-LEUCYLAMIDO-[4-GUANIDINO]BUTANE[L-3-TRANS-CARBOXY-OXIRAN-2-CARBONYL]-LEU-AGMATIN;(L-3-trans-carboxyoxiran-2-carbonyl)-L-leucyl-agmatin;E-64 HEMIHYDRATE;E-64 PROTEASE INHIBITOR;e64(proteinaseinhibitor);E-64,L-trans-Epoxysuccinyl-Leu-agMatine;EPOXYSUCCINYL-L-LEUCYLAMIDO-(4-GUANIDINO)BUTANE;L-TRANS-EPOXYSUCCINYL-LEU-AGMATINE;proteinaseinhibitore64;thiolproteaseinhibitor;L-trans-3-Carboxyoxiran-2-carbonyl-L-leucylagmatine;n-[n-(l-3-trans-carboxirane-2-carbonyl)-l-leucyl]-4-aminobutylguanidine;n-[n-(l-3-trans-carboxirane-2-carbonyl)-l-leucyl]-agmatine. note: another name for l-3-trans-carboxyoxiran-2-carboxylic acid acid is l-transepoxysuccinic acid. agmatine is 4-aminobutylguanidine.;n-[n-( l-transepoxysuccinic acid)-l-leucyl]-agmatine

Cas No.

66701-25-5

分子式

C₁₅H₂₇N₅O₅

分子量

357.41

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

E-64 (Proteinase inhibitor E 64) is a potent irreversible inhibitor against general cysteine proteases with IC₅₀ of 9 nM for papain.

性状

Solid

IC50 & Target[1][2]

IC50: 9 nM (Papain)

体外研究(In Vitro)

E-64 (Proteinase inhibitor E 64) is a cathepsin B-specific inhibitor, and its binding modes with papain, actinidin, cathepsin L, and cathepsin K have been reviewed at the atomic level. E-64 has been widely used as a potent and irreversible (covalent-type) inhibitor for many cysteine proteases such as papain, ficin, actinidin, cathepsin B and L. The S.cervi adult parasites are incubated in the Krebs Ringer bicarbonate (KRB) maintenance medium for 8 h at 37°C, 5% CO₂ with 5, 10, 20 and 40 μM concentration of E-64. E-64 shows a concentration and time dependent decrease in motility and viability of the parasites (EC₅₀=16 μM).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

A broad spectrum of expression of CD4 and CD19 is found exists in both the islets and pancreatic lymph nodes (PLNs) and that anti-serpin B13 mAb exposure causes a significant shift that favored cells expressing low-to-intermediate amounts of these markers. However, this shift is abolished in animals that receive anti-serpin B13 mAb in the presence of the protease inhibitor E-64 (Proteinase inhibitor E 64), which maintains its blocking activity under the experimental conditions used. Dahl salt-sensitive (SS) rats are fed an 8% high salt NaCl diet and intravenously infused with the irreversible cysteine cathepsin inhibitor E-64 (1 mg/day) or the vehicle (control). Both the control and E-64 infused groups develope significant hypertension and kidney damage, and no difference of the mean arterial pressure and the hypertension-associated albuminuria is observed between the groups.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Matsumoto K, et al. Structural basis of inhibition of cysteine proteases by E-64 and its derivatives. Biopolymers. 1999;51(1):99-107. [Information]

[2]. Wadhawan M, et al. Inhibition of cathepsin B by E-64 induces oxidative stress and apoptosis in filarial parasite. PLoS One. 2014 Mar 25;9(3):e93161. [Information]

[3]. Baldzizhar R, et al. Anti-serpin antibody-mediated regulation of proteases in autoimmune diabetes. J Biol Chem. 2013 Jan 18;288(3):1612-9. [Information]

[4]. Blass G, et al. Chronic cathepsin inhibition by E-64 in Dahl salt-sensitive rats. Physiol Rep. 2016 Sep;4(17). pii: e12950. [Information]

溶解度数据

体外研究:

DMSO : 62.5 mg/mL (174.87 mM; Need ultrasonic)

H₂O : 5 mg/mL (13.99 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7979 mL	13.9895 mL	27.9791 mL
5 mM	0.5596 mL	2.7979 mL	5.5958 mL
10 mM	0.2798 mL	1.3990 mL	2.7979 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： PBS
Solubility: 50 mg/mL (139.90 mM); Clear solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMSO 90% saline
Solubility: ≥ 2.5 mg/mL (6.99 mM); Clear solution
3.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.82 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
4.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.82 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
5.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.82 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

搜索质检报告(COA)

产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

相关产品

The molarity calculator equation

The dilution calculator equation