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Calpain Inhibitor I, ALLN (Synonyms: AcLeuLeuNleAldehyde, ALLN, MG 101)

カタログ番号GC12527

非選択的システインプロテアーゼ阻害剤

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Calpain Inhibitor I, ALLN 化学構造

Cas No.: 110044-82-1

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$60.00
在庫あり
5mg
$39.00
在庫あり
25mg
$119.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

DLD1-TRAIL/R cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

0, 10, 20 and 50 μM; 96 hrs

Applications

In DLD1-TRAIL/R cells, Calpain Inhibitor I combined with Ad/gTRAIL induced cell death dramatically while Calpain Inhibitor I or Ad/gTRAIL alone only had minimal killing effects.

Animal experiment [2]:

Animal models

Splanchnic artery occlusion (SAO)-shocked rats

Dosage form

15 mg/kg; i.p.

Applications

Calpain Inhibitor I, given intraperitoneally 30 mins before ischemia at a dose of 15 mg/kg, significantly reduced IκB-α degradation, the intensity of P-selectin/ICAM-1 in the reperfused ileum, neutrophil infiltration as well as malondialdehyde levels. Meanwhile, pretreatment of Calpain Inhibitor I markedly improved mean arterial blood pressure and the histological status of the reperfused tissue.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Zhu H1, Zhang L, Huang X, Davis JJ, Jacob DA, Teraishi F, Chiao P, Fang B. Overcoming acquired resistance to TRAIL by chemotherapeutic agents and calpain inhibitor I through distinct mechanisms. Mol Ther.?2004 May;9(5):666-73.

[2]. Marzocco S1, Di Paola R, Autore G, Mazzon E, Pinto A, Caputi AP, Thiemermann C, Cuzzocrea S. Calpain inhibitor I reduces intestinal ischemia-reperfusion injury in the rat. Shock. 2004 Jan;21(1):38-44.

Background

カルペイン阻害剤Iは、それぞれKi値が190 nM、220 nM、150 nM、および500 pMのカルペインI、カルペインII、カテプシンBおよびカテプシンLの阻害剤です。

Calpain阻害剤IをAd/gTRAILと組み合わせることで、DLD1-TRAIL/R細胞において細胞死が劇的に誘導されました。一方、単独のcalpainは殺傷効果がほとんどありませんでした。Calpain阻害剤IとTRAILタンパク質の組み合わせは、caspase-8およびcaspase-3の両方を活性化サブユニットに切断する結果をもたらしました[1]。

カルペイン阻害剤を投与した雄性スプラグ・ドーリー ラットでは、P-セレクチン/ICAM-1の発現、好中球浸潤、脂質過酸化、ニトロチロシン、PAR形成およびIκB-αの分解が減少することが観察されました[2]。

Reference:
[1] Zhu H1, Zhang L, Huang X, Davis JJ, Jacob DA, Teraishi F, Chiao P, Fang B. Overcoming acquired resistance to TRAIL by chemotherapeutic agents and calpain inhibitor I through distinct mechanisms. Mol Ther. 2004 May;9(5):666-73.
[2] Marzocco S1, Di Paola R, Autore G, Mazzon E, Pinto A, Caputi AP, Thiemermann C, Cuzzocrea S.  Calpain inhibitor I reduces intestinal ischemia-reperfusion injury in the rat. Shock. 2004 Jan;21(1):38-44.

Chemical Properties

Cas No. 110044-82-1 SDF
同義語 AcLeuLeuNleAldehyde, ALLN, MG 101
Chemical Name 2-acetamido-4-methyl-N-[4-methyl-1-oxo-1-(1-oxohexan-2-ylamino)pentan-2-yl]pentanamide
Canonical SMILES CCCCC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C
Formula C20H37N3O4 M.Wt 383.54
溶解度 ≥ 19.1mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.6073 mL 13.0364 mL 26.0729 mL
5 mM 0.5215 mL 2.6073 mL 5.2146 mL
10 mM 0.2607 mL 1.3036 mL 2.6073 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Review for Calpain Inhibitor I, ALLN

Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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