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Aloxistatin

Aloxistatin

产品编号 T6040   CAS 88321-09-9
别名: E64d, Loxistatin, 阿洛司他丁, E64c ethyl ester

Aloxistatin (E64d) 是一种不可逆的、可透过膜的溶酶体和细胞溶质半胱氨酸蛋白酶抑制剂,能够抑制完整血小板中的钙蛋白酶活性。它是一种半胱氨酸蛋白酶抑制剂,具有血小板聚集抑制活性。

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Aloxistatin Chemical Structure
Aloxistatin, CAS 88321-09-9
规格 价格/CNY 货期 数量
1 mg ¥ 313 现货
2 mg ¥ 476 现货
5 mg ¥ 842 现货
10 mg ¥ 1,470 现货
25 mg ¥ 2,530 现货
50 mg ¥ 3,730 现货
100 mg ¥ 5,290 现货
500 mg ¥ 10,800 现货
1 mL * 10 mM (in DMSO) ¥ 877 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: Aloxistatin (T6040)
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纯度: 99.47%
纯度: 99.46%
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生物活性
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存储 & 溶解度
参考文献
产品描述 Aloxistatin (E64d) is an inhibitor of cysteine protease with blood platelet aggregation inhibiting activity. Aloxistatin is an irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases with the ability to inhibit calpain activity in intact platelets.
体外活性 Aloxistatin can enter the intact platelet and inhibit proteolysis by inhibiting calpain. [2] Aloxistatin blunts Parathyroid hormone (PTH)-induced cell proliferation and inhibits differentiation osteoblasts in vitro. [3]
体内活性 Aloxistatin (100 mg/kg, p.o.) strongly inhibits the cathepsin B&L activities in the skeletal muscle, heart and liver of hamsters. [1] In spinal cord injury (SCI) rats, Aloxistatin provides neuroprotection in SCI lesion and penumbra. [4] Aloxistatin reduces brain amyloid-β and improves memory deficits in Alzheimer's disease animal models by inhibiting cathepsin B activity. [5]
激酶实验 The CTLs and NK cells (0.8×106/mL) are treated with the inhibitors L1 (10-20 μM) or Aloxistatin (20-30 μM) for 24 hr at 37°C in 24-well plates. Cells are then used in 51Cr-release assays or are lysed to examine perforin in Western blots. The inhibitor is also added at the same concentration during the 4 hr reactions in some 51Cr-release assays, as indicated. Cell lysates are prepared using NP-40 lysis buffer (25 mM HEPES, 250 mM NaCl, 2.5 mM ethylenediaminetetraacetic acid, 0.1% volume/volume Nonidet P-40) and total protein concentration is determined using the Bradford assay. Equal amounts of protein are loaded and resolved on 8% SDS-PAGE gels. Human or mouse perforin is detected using the appropriate antibodies as indicated. Anti-actin antibody is used as a loading control[2].
细胞实验 Aloxistatin (E64d) is dissolved in DMSO and stored, and then diluted with appropriate medium (final DMSO 0.1 %) before use[3]. Cell proliferation and apoptosis are assessed by staining for a proliferation marker, Ki67, or an apoptotic marker, cleaved caspase 3, following the protocol described above for the polarity markers. MCF10 variants are grown in 3D rBM overlay cultures for 4 days and are treated with 0.1 % DMSO, 5 μM CA074Me or 5 μM Aloxistatin. The percentage of structures that are positive for Ki67 or cleaved caspase 3 is determined by counting a total of 100 structures on two separate coverslips with a Zeiss Axiophot epifluorescent microscope. Structures are considered Ki67 positive if they contained at least one cell staining for Ki67. Structures are considered to be caspase 3 positive if they contained at least one cell that is positive for cleaved caspase 3 and the positive cell(s) is not localized in the center of a developing lumen[3].
别名 E64d, Loxistatin, 阿洛司他丁, E64c ethyl ester
分子量 342.43
分子式 C17H30N2O5
CAS No. 88321-09-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 6.9 mg/mL (20 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9203 mL 14.6015 mL 29.203 mL 73.0076 mL
5 mM 0.5841 mL 2.9203 mL 5.8406 mL 14.6015 mL
10 mM 0.292 mL 1.4602 mL 2.9203 mL 7.3008 mL
20 mM 0.146 mL 0.7301 mL 1.4602 mL 3.6504 mL

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TargetMol Library Books参考文献

1. Tamai M, et al. J Pharmacobiodyn. 1986, 9(8), 672-677. 2. McGowan EB, et al. Biochem Biophys Res Commun. 1989, 158(2), 432-435. 3. Murray EJ, et al. Metabolism. 1997 , 46(9), 1090-1094. 4. Ray SK, et al. Ann N Y Acad Sci. 2001, 939, 436-449. 5. Hook G, et al. J Alzheimers Dis. 2011, 26(2), 387-408.
Simeprevir Glecaprevir MM3122 Tipranavir Setrobuvir Z-FA-FMK SSAA09E3 Ivermectin B1a

相关化合物库

该产品包含在如下化合物库中:
高选择性抑制剂库 抑制剂库 表型筛选靶点鉴定库 抗衰老化合物库 ReFRAME 相关化合物库 人代谢物化合物库 抗感染化合物库 共价抑制剂库 NO PAINS 化合物库 已知活性化合物库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Aloxistatin 88321-09-9 Microbiology/Virology Proteases/Proteasome SARS-CoV Cysteine Protease Cathepsin Inhibitor inhibit E64d Loxistatin 阿洛司他丁 E64c ethyl ester SARS coronavirus inhibitor

 

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