Aloxistatin (E64d)

製品コードS7393 バッチS739301

印刷

化学情報

 Chemical Structure 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
* <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 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]

in vivo

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]

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 the drug 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.

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:

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
A bat MERS-like coronavirus circulates in pangolins and utilizes human DPP4 and host proteases for cell entry [ Cell, 2023, 186(4):850-863.e16] PubMed: 36803605
Differences in syncytia formation by SARS-CoV-2 variants modify host chromatin accessibility and cellular senescence via TP53 [ Cell Rep, 2023, 42(12):113478] PubMed: 37991919
Canine distemper virus N protein induces autophagy to facilitate viral replication [ BMC Vet Res, 2023, 19(1):60] PubMed: 36922800
Babesia divergens egress from host cells is orchestrated by essential and druggable kinases and proteases [ Res Sq, 2023, rs.3.rs-2553721] PubMed: 36909484
Spike-mediated ACE2 down-regulation was involved in the pathogenesis of SARS-CoV-2 infection [ J Infect, 2022, S0163-4453(22)00404-2] PubMed: 35793758
RNF43G659fs is an oncogenic colorectal cancer mutation and sensitizes tumor cells to PI3K/mTOR inhibition [ Nature Communications, 2022, 3181-2022)] PubMed: None
RNF43 G659fs is an oncogenic colorectal cancer mutation and sensitizes tumor cells to PI3K/mTOR inhibition [ Nat Commun, 2022, 13(1):3181] PubMed: 35676246
Mannose ameliorates experimental colitis by protecting intestinal barrier integrity [ Nat Commun, 2022, 13(1):4804] PubMed: 35974017
Oncolytic peptide LTX-315 induces anti-pancreatic cancer immunity by targeting the ATP11B-PD-L1 axis [ J Immunother Cancer, 2022, 10(3)e004129] PubMed: 35288467

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。