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
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 110044-82-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. |
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.
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. |
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
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