Aloxistatin (E64d)

製品コードS7393 バッチS739301

印刷

化学情報

Synonyms

E-64d

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₇H₃₀N₂O₅

分子量

342.43

CAS No.

88321-09-9

Solubility (25°C)*

体外

DMSO

68 mg/mL (198.58 mM)

Ethanol

68 mg/mL (198.58 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Aloxistatin (E64d) is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry, and aloxistatin treatment reduced cellular entry of SARS-CoV-2 pseudovirions by 92.3%.
in vitro	Aloxistatin (E64d) can enter the intact platelet and inhibit proteolysis by inhibiting calpain. ^[2] It blunts Parathyroid hormone (PTH)-induced cell proliferation and inhibits differentiation osteoblasts in vitro. ^[3]
in vivo	Aloxistatin (E64d) (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, it provides neuroprotection in SCI lesion and penumbra. ^[4] This compound reduces brain amyloid-β and improves memory deficits in Alzheimer's disease animal models by inhibiting cathepsin B activity. ^[5]

製品説明

Aloxistatin (E64d) is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry, and aloxistatin treatment reduced cellular entry of SARS-CoV-2 pseudovirions by 92.3%.

in vitro

Aloxistatin (E64d) can enter the intact platelet and inhibit proteolysis by inhibiting calpain. ^[2]

It blunts Parathyroid hormone (PTH)-induced cell proliferation and inhibits differentiation osteoblasts in vitro. ^[3]

in vivo

Aloxistatin (E64d) (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, it provides neuroprotection in SCI lesion and penumbra. ^[4]

This compound reduces brain amyloid-β and improves memory deficits in Alzheimer's disease animal models by inhibiting cathepsin B activity. ^[5]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	NCM460 cells
	濃度	1 μM
	反応時間	24 h
	実験の流れ	Cells were treated with indicated concentration of Aloxistatin (E64d) for 24 hour.
動物実験	動物モデル	Hamsters
	投薬量	~100 mg/kg
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/3023601/
https://pubmed.ncbi.nlm.nih.gov/2537073/
https://pubmed.ncbi.nlm.nih.gov/9284902/

https://pubmed.ncbi.nlm.nih.gov/11462799/
https://pubmed.ncbi.nlm.nih.gov/21613740/
https://pubmed.ncbi.nlm.nih.gov/35974017/

+ 展开

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Enzymatic combinatorial synthesis of E-64 and related cysteine protease inhibitors [ Nat Chem Biol, 2025, 10.1038/s41589-025-01907-2]	PubMed: 40346252
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The phagosome-mediated anti-bacterial immunity is governed by the proton-activated chloride channel in peritoneal macrophages [ bioRxiv, 2025, 2025.02.27.640612]	PubMed: 40060571
Truncating NFKB1 variants cause combined NLRP3 inflammasome activation and type I interferon signaling and predispose to necrotizing fasciitis [ Cell Rep Med, 2024, 5(4):101503]	PubMed: 38593810
OTULIN confers cisplatin resistance in osteosarcoma by mediating GPX4 protein homeostasis to evade the mitochondrial apoptotic pathway [ J Exp Clin Cancer Res, 2024, 43(1):330]	PubMed: 39721999
Retinoic acid alleviates rotavirus-induced intestinal damage by regulating redox homeostasis and autophagic flux in piglets [ Anim Nutr, 2024, 20:16:409-421.]	PubMed: 38371474
Retinoic acid alleviates rotavirus-induced intestinal damage by regulating redox homeostasis and autophagic flux in piglets [ Anim Nutr, 2024, 16:409-421]	PubMed: 38371474
SARS-CoV-2 Omicron subvariants progressively adapt to human cells with altered host cell entry [ mSphere, 2024, 9(9):e0033824]	PubMed: 39191389
Unveiling the Role of TMPRSS2 in the Proteolytic Activation of Pandemic and Zoonotic Influenza Viruses and Coronaviruses in Human Airway Cells [ Viruses, 2024, 16(11)1798]	PubMed: 39599912
Lotus Sprout Extract Induces Selective Melanosomal Autophagy and Reduces Pigmentation [ J Cosmet Dermatol, 2024, 10.1111/jocd.16587]	PubMed: 39305105

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。