Calpeptin

製品コードS7396 バッチS739604

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H30N2O4
分子量 362.46 CAS No. 117591-20-5
Solubility (25°C)* 体外 DMSO 72 mg/mL (198.64 mM)
Ethanol 72 mg/mL (198.64 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5% DMSO 95% Corn oil
0.6mg/ml Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.6mg/ml Taking the 1 mL working solution as an example, add 50 μL of 72 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 Calpeptin is a potent, cell-permeable calpain inhibitor with ID50 of 52 nM, 34 nM, 138 nM, and 40 nM for Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papainb, and Calpain I (human platelets), respectively. Calpeptin attenuates apoptosis and intracellular inflammatory changes in muscle cells.
in vitro Calpeptin inhibits 20K phosphorylation in a dose-related manner in platelets stimulated by thrombin, ionomycin or collagen. [1] In differentiating PC12 cells, Calpeptin promotes neurite elongation via inhibition of Calpain activity. [2] In rat retinal ganglion cells, Calpeptin attenuates apoptosis, maintains normal whole-cell membrane potential, and thus provides functional neuroprotection. [3]
in vivo In a feline right ventricular (RV) PO (RVPO) model, calpeptin (0.6 mg/kg, i.v.) blocks the activation of calpain and caspase-3, cleavage of their substrates, and cardiomyocyte programmed cell death. [4] In a rat focal cerebral ischemia–reperfusion injury model, Calpeptin reduces the neuronal apoptosis in hippocampal CA1 sector via inhibition of the expression of Caspase-3. [5]

プロトコル(参考用のみ)

キナーゼアッセイ Enzyme assay
The activity of calpain I and II from porcine is assayed using 0.4% casein as a substrate in 50 mM imidazole-HCl (pH 7.2), 5 mM cysteine and 1 mM CaCl2. After incubation at 30°C for 30 min, the reaction is stopped by adding trichloroacetic acid and the acid-soluble products in the filtrate are measured at 950 nm. One unit of calpain is defined the amount of enzyme which increases the absorbance by 1.0 at 750 nm. The activity of platelet calpain is assayed using 0.5% casein as a substrate in 100 mM imidazole-HCl (pH 6.9), 50 mM KCI, 1 mM DTT and 2 mM CaCl2. The reaction is terminated by the mixture of 0.11M CCI3COOH, 0.22 M CH3COONa and 0.33 M CH3COOH, after 20 min at 25°C. The acid- soluble products are determined using fluorescamine. One unit of platelet calpain activity is defined as the amount of enzyme which liberate 1 μmol of α-amino group as leucine equivalent per hour. The assay for papain, trypsin and chymotrypsin is measured using casein as a substrate. After incubating at 35°C for 20 min, the reaction is stopped by 5% trichloroacetic acid. The absorbance at 280 nm of the acid-soluble products are read against the blank. One unit of papain activity hydrolyzes 1 μmol of N2-benzoyl-L-arginine ethyl ester (BAEE) per minute at pH 6.2 at 25°C. The amidolytic activity of thrombin is measured using S-2238. The enzymatic activity of thrombin against fibrinogen in plasma is assayed by a visual estimation of clotting time using a Clotek.
動物実験 動物モデル Feline right ventricular (RV) PO (RVPO) model
投薬量 0.6 mg/kg
投与方法 i.v.

カスタマーフィードバック

Data from [Data independently produced by , , Oncol Rep, 2017, 37(6):3651-3659]

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：

Defined extracellular matrix compositions support stiffness-insensitive cell spreading and adhesion signaling [ Proc Natl Acad Sci U S A, 2023, 120(43):e2304288120] PubMed: 37844244
Defined extracellular matrix compositions support stiffness-insensitive cell spreading and adhesion signaling [ Proc Natl Acad Sci U S A, 2023, 120(43):e2304288120] PubMed: 37844244
The mechanosensitive TRPV2 calcium channel promotes human melanoma invasiveness and metastatic potential [ EMBO Rep, 2023, e55069.] PubMed: 36744297
The lactate-NAD+ axis activates cancer-associated fibroblasts by downregulating p62 [ Cell Rep, 2022, 39(6):110792] PubMed: 35545049
Polysaccharides from Polygonatum cyrtonema Hua Reduce Depression-Like Behavior in Mice by Inhibiting Oxidative Stress-Calpain-1-NLRP3 Signaling Axis [ Oxid Med Cell Longev, 2022, 2022:2566917] PubMed: 35498131
Calpain-1: a Novel Antiviral Host Factor Identified in Porcine Small Intestinal Mucus [ mBio, 2022, 13(5):e0035822] PubMed: 36102516
Potential drug discovery for COVID-19 treatment targeting Cathepsin L using a deep learning-based strategy [ Comput Struct Biotechnol J, 2022, 20:2442-2454] PubMed: 35602976
Berberine alleviates liver fibrosis through inducing ferrous redox to activate ROS-mediated hepatic stellate cells ferroptosis [ Cell Death Discov, 2021, 7(1):374] PubMed: 34864819
Xanthohumol Is a Potent Pan-Inhibitor of Coronaviruses Targeting Main Protease [ Int J Mol Sci, 2021, 22(22)12134] PubMed: 34830015
Caspase-mediated cleavage of miRNA processing proteins Drosha, DGCR8, Dicer, and TRBP2 in heat-shocked cells and its inhibition by HSP70 overexpression [ Cell Stress Chaperones, 2021, 10.1007/s12192-021-01242-0] PubMed: 34719748

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。

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