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E-64d/阿洛司他丁 {[allProObj[0].p_purity_real_show]}

货号:A162425 同义名: E64c ethyl ester; Aloxistatin

E-64d(E64d)是一种细胞可渗透、不可逆的广谱半胱氨酸蛋白酶抑制剂,对MERS-CoV具有入侵阻断作用。

E-64d/阿洛司他丁 化学结构 CAS号:88321-09-9
E-64d/阿洛司他丁 化学结构
CAS号:88321-09-9
E-64d/阿洛司他丁 3D分子结构
CAS号:88321-09-9
E-64d/阿洛司他丁 化学结构 CAS号:88321-09-9
E-64d/阿洛司他丁 3D分子结构 CAS号:88321-09-9
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E-64d/阿洛司他丁 纯度/质量文件 产品仅供科研

货号:A162425 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Cysteine Protease 其他靶点 纯度
Z-FA-FMK 99%+
Leupeptin hemisulfate 97%
PMSF 95%
PD 151746 +

μ-Calpain, IC50: 260 nM

m-calpain, IC50: 5.33 μM

98%
Odanacatib ++++

Cathepsin K (human), IC50: 0.2 nM

Cathepsin K (rabbit), IC50: 1 nM

99%+
E-64 +++

Cysteine protease, IC50: 9 nM

99%+
E 64c 95%
E-64d 99%+
MG-101 98%+
Calpeptin ++

Calpain I (porcine erythrocytes), ID50: 52 nM

Calpain II (porcine kidney), ID50: 40 nM

98%+
Cathepsin inhibitor 1 +++

Cathepsin L, pIC50: 7.9

Cathepsin L2, pIC50: 5.5

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

E-64d/阿洛司他丁 生物活性

靶点
  • Cysteine Protease

描述 Cysteine proteases play multiple roles in basically all aspects of physiology and development. Furthermore, they are engaged in signalling pathways and in the response to biotic and abiotic stresses[3]. Aloxistatin is a specific and potent inhibitor of cysteine proteinases isolated from a culture of Aspergillus japonicus[3]. Aloxistatin at a series of concentrations was able to enter the intact platelet and inhibit the protease activity in lysed platelets when incubated for 5 min[4]. After a brief preincubation with the membrane-permeable, Aloxistatin (10 mg/ml) blunted PTH-induced (parathyroid hormone) cell proliferation in sub-confluent cultures and also attenuated proliferation and inhibited differentiation in longer-term confluent cultures[5]. Aloxistatin(100 mg/kg, p.o.) inhibited the activity of cathepsin B&L in skeletal muscle, heart, and liver of hamsters[6].
作用机制 Aloxistatin reacts irreversibly with the thiol group at the active site.

E-64d/阿洛司他丁 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 数据源
U937 cells Function assay Blockade of cathepsin G processing in human U937 cells by densitometry, IC50=1.1 μM 17535802

E-64d/阿洛司他丁 参考文献

[1]Wilkesman J. Cysteine Protease Zymography: Brief Review. Methods Mol Biol. 2017;1626:25-31. doi: 10.1007/978-1-4939-7111-4_3. PMID: 28608197.

[2]McGowan EB, Becker E, Detwiler TC. Inhibition of calpain in intact platelets by the thiol protease inhibitor E-64d. Biochem Biophys Res Commun. 1989 Jan 31;158(2):432-5. doi: 10.1016/s0006-291x(89)80065-8. PMID: 2537073.

[3]Murray EJ, Grisanti MS, Bentley GV, Murray SS. E64d, a membrane-permeable cysteine protease inhibitor, attenuates the effects of parathyroid hormone on osteoblasts in vitro. Metabolism. 1997 Sep;46(9):1090-4. doi: 10.1016/s0026-0495(97)90284-5. PMID: 9284902.

[4]Tamai M, Matsumoto K, Omura S, Koyama I, Ozawa Y, Hanada K. In vitro and in vivo inhibition of cysteine proteinases by EST, a new analog of E-64. J Pharmacobiodyn. 1986 Aug;9(8):672-7. doi: 10.1248/bpb1978.9.672. PMID: 3023601.

E-64d/阿洛司他丁 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.92mL

0.58mL

0.29mL

14.60mL

2.92mL

1.46mL

29.20mL

5.84mL

2.92mL

E-64d/阿洛司他丁 技术信息

CAS号88321-09-9
分子式C17H30N2O5
分子量 342.43
SMILES Code O=C([C@H]1O[C@@H]1C(N[C@@H](CC(C)C)C(NCCC(C)C)=O)=O)OCC
MDL No. MFCD00132883
别名 E64c ethyl ester; Aloxistatin; ethyl ester Loxistatin; NSC 694281; Loxistatin; EST; EP 453
运输蓝冰
InChI Key SRVFFFJZQVENJC-IHRRRGAJSA-N
Pubchem ID 65663
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

DMSO: 120 mg/mL(350.44 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

无水乙醇: 30 mg/mL(87.61 mM),注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 36 mg/mL suspension

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