阿洛司他丁|88321-09-9|(阿洛司他丁; E64d; E64c ethyl ester)-陌孚医药/Medlife

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阿洛司他丁 (Synonyms: 阿洛司他丁; E64d; E64c ethyl ester)

目录号: PC15607 纯度: ≥98%

CAS No. :88321-09-9

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PC15607-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥1911.00	请登录

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中文名称

阿洛司他丁

中文别名

Aloxistatin 抑制剂;E-64d蛋白酶抑制剂,阿洛司他丁;L-反式-环氧丁二酰基-Leu-3-甲基丁胺乙酯;阿洛司他丁;氯苯胺灵;氯普芬;(2S,3S)-3-[[(2S)-4-甲基-1-[(3-甲基丁基)氨基]-1-氧代-2-戊基]氨基甲酰基]-2-环氧乙烷甲酸乙酯

英文名称

Aloxistatin

英文别名

2-Oxiranecarboxylicacid,3-[[[(1S)-3-methyl-1-[[(3-methylbutyl)amino]carbonyl]butyl]amino]carbonyl]-,ethyl ester, (2S,3S)-;E-64d [for Biochemical Research];E-64d;(2S,3S)-3-[[[(1S)-3-Methyl-1-[[(3-methylbutyl)amino]carbonyl]-butyl]amino]carbonyl]-2-oxiranecarboxylic acid ethyl ester;2-Oxiranecarboxylicacid,3-[[[(1S)-3-methyl-1-[[(3-methylbutyl)amino]carbonyl]butyl]amino]carbo...;ALLATOSTATIN I;Aloxistatin;E 64d;E-64-d;E-64d (EST,EP 453,NSC 694281, Aloxistatin);EST;L-trans-Epoxysuccinyl-Leu-3-methylbutylamide-ethyl ester;Aloxistatin (E-64d) EST Loxistatin;E64c ethyl ester;ep453;LOXASTATIN;LOXISTATIN;(2S,3S)-trans-Epoxysuccinyl-L-leucylamido-3-methylbutane ethyl ester;Ethyl (2S,3S)-3-[[(2S)-4-Methyl-1-[(3-methylbutyl)amino]-1-oxo-2-pentanyl]carbamoyl]-2-oxiranecarboxylate;(2S,3S)-3-[[(2S)-4-Methyl-1-[(3-methylbutyl)amino]-1-oxo-2-pentanyl]carbamoyl]-2-oxiranecarboxylic Acid Ethyl Ester;Aloxistatine;Aloxistatinum;Aloxistatina;Aloxistatin [INN];E 64c ethyl ester;EST (pharmaceutical);Aloxistatine [French];Aloxistatinum [Latin];Aloxistatina [Spanish];C17H30N2O5;EP 453;E64d;L5W337AOUR;MLS000028372;SMR000058552;Ethyl (+)-(2S,3S)-2,3-epoxy-N-((S)-1-(isopentylcarbamoyl)-3-methylbutyl)succinamate;Oxiranecarb

Cas No.

88321-09-9

分子式

C₁₇H₃₀N₂O₅

分子量

342.43

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

Aloxistatin (E64d) is a cell-permeable and irreversible broad-spectrum cysteine protease inhibitor. Aloxistatin (E64d) exhibits entry-blocking effect for MERS-CoV.

性状

Solid

IC50 & Target[1][2]

Cysteine protease

体外研究(In Vitro)

Inhibition of protease-resistant prion protein (PrP-res) accumulation in ScNB cells by cysteine protease inhibitor Aloxistatin (E64d) with IC₅₀ of 0.5±0.11 μM. For the cell surface PrP-sen detection, PrP-sen is immunoprecipitated from media treated with phosphatidylinositol-specific phospholipase C (PIPLC) to release pulse-S-labeled PrP-sen from the cell surface. Aloxistatin is maintained at 15 μM, respectively, in the labeling media of all but the control cells . Aloxistatin (E64d) (which specifically blocks cysteine proteases, but not serine proteases such as granzymes) is able to completely block turnover of the CatL substrate Z-Phe-Arg-aminomethylcoumarin, when pre-incubated with NK-92 or YT 5 cells. Aloxistatin (E64d) is a broad-spectrum cell-permeable inhibitor of cysteine proteases.

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

体内研究(In Vivo)

Oral administration of Aloxistatin (E64d) to guinea pigs results in a dose-dependent reduction in brain, CSF and plasma Aβ(40) and Aβ(42). Aloxistatin also causes a biphasic dose-dependent reduction in brain CTFβ. Aloxistatin causes a dose-dependent increase in brain sAβPPα. The mean sAβPPα levels are significantly higher than the no dose group for Aloxistatin doses of 5 mg/kg/day or greater with the highest Aloxistatin dose resulting in the maximum increase in sAβPPα of about 54% more than the control group. Similar to the Aβ effect, oral Aloxistatin administration produces a biphasic dose-dependent reduction in brain cathepsin B activity. The minimum effective dose is about 1 mg/kg/day with the highest Aloxistatin dose causing the maximum reduction in brain cathepsin B activity of about 91% lower than that of the control group. Thus, Aloxistatin reduces guinea pig brain cathepsin B activity in a manner which is consistent with the compound inhibiting cathepsin B β-secretase activity. Aloxistatin (E64d) inhibits the increases in the expression of AT_1AR and ACE genes in rats. Administration of RNH-6270 or Aloxistatin reduces the increase in the superoxide production of the intramyocardial coronary arteries in HF rats.

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]. Doh-Ura K, et al. Lysosomotropic agents and cysteine protease inhibitors inhibit scrapie-associated prion protein accumulation. J Virol. 2000 May;74(10):4894-7. [Information]

[2]. Konjar S, et al. Human and mouse perforin are processed in part through cleavage by the lysosomal cysteine proteinase cathepsin L. Immunology. 2010 Oct;131(2):257-67. [Information]

[3]. Mullins SR, et al. Three-dimensional cultures modeling premalignant progression of human breast epithelial cells: role of cysteine cathepsins. Biol Chem. 2012 Dec;393(12):1405-16. [Information]

[4]. Hook G, et al. The cysteine protease inhibitor, E64d, reduces brain amyloid-β and improves memory deficits in Alzheimers disease animal models by inhibiting cathepsin B, but not BACE1, β-secretase activity. J Alzheimers Dis. 2011;26(2):387-408. [Information]

[5]. Cheng XW, et al. Superoxide-dependent cathepsin activation is associated with hypertensive myocardial remodeling and represents a target for angiotensin II type 1 receptor blocker treatment. Am J Pathol. 2008 Aug;173(2):358-69. [Information]

[6]. 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. [Information]

溶解度数据

体外研究:

DMSO : 250 mg/mL (730.08 mM; Need ultrasonic)

Ethanol : ≥ 33.33 mg/mL (97.33 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9203 mL	14.6015 mL	29.2030 mL
5 mM	0.5841 mL	2.9203 mL	5.8406 mL
10 mM	0.2920 mL	1.4602 mL	2.9203 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： 10% EtOH 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (7.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.30 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 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
2.

建议依照次序添加每种溶剂： 10% EtOH 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (7.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.30 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 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
3.

建议依照次序添加每种溶剂： 10% EtOH 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (7.30 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 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中，混合均匀。
4.

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 (6.07 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (6.07 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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
5.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (6.07 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.07 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。

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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。

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