Calpeptin

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Calpeptin

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	117591-20-5
规格:	≥98%

包装与价格：

包装	价格(元)
10mg	电议
25mg	电议
50mg	电议
100mg	电议
250mg	电议
500mg	电议

产品介绍

Calpeptin (sequence: Z-Leu-nLeu-H) is a novel, potent, cell-permeable calpain inhibitor with anti-fibrotic activity. It inhibits Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papainb, and Calpain I (human platelets) with IC50s of 52 nM, 34 nM, 138 nM, and 40 nM, respectively. It attenuates apoptosis and inflammation, cell death, and axonal damage in animal model of multiple sclerosis. Calpeptin also reduced both angiopoietin-1-dependent migration and IL-6-dependent proliferation of the cells, which could be the underlying mechanism of the preventive effect of Calpeptin on pulmonary fibrosis.

理化性质和储存条件

Molecular Weight (MW)	362.46
Formula	C20H30N2O4
CAS No.	117591-20-5
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 72 mg/mL (198.6 mM)
	Water:<1 mg/mL
	Ethanol: 72 mg/mL (198.6 mM)
SMILES	O=C(OCC1=CC=CC=C1)N[C@H](C(N[C@H](C=O)CCCC)=O)CC(C)C
Synonyms	Calpain; Benzylcarbonyl-leu-nleu-H; N-Cbz-leu-nleu-al. Chemical Name: benzyl ((S)-4-methyl-1-oxo-1-(((S)-1-oxohexan-2-yl)amino)pentan-2-yl)carbamate InChi Key: PGGUOGKHUUUWAF-ROUUACIJSA-N InChi Code: InChI=1S/C20H30N2O4/c1-4-5-11-17(13-23)21-19(24)18(12-15(2)3)22-20(25)26-14-16-9-7-6-8-10-16/h6-10,13,15,17-18H,4-5,11-12,14H2,1-3H3,(H,21,24)(H,22,25)/t17-,18-/m0/s1

实验参考方法

In Vitro	In vitro activity: Calpeptin inhibits 20K phosphorylation in a dose-related manner in platelets stimulated by thrombin, ionomycin or collagen. In differentiating PC12 cells, Calpeptin promotes neurite elongation via inhibition of Calpain activity. In rat retinal ganglion cells, Calpeptin attenuates apoptosis, maintains normal whole-cell membrane potential, and thus provides functional neuroprotection Kinase Assay: Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets Cell Assay: Calpeptin reduced production of TGF-b1, IL-6, angiopoietin-1 and collagen synthesis from lung fibroblasts. Calpeptin also reduced both angiopoietin-1-dependent migration and IL-6-dependent proliferation of the cells, which could be the underlying mechanism of the preventive effect of Calpeptin on pulmonary fibrosis.
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. 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.
Animal model	Feline right ventricular (RV) PO (RVPO) model
Formulation & Dosage	Dissolved in 1% DMSO in saline; 0.6 mg/kg; i.v. injection
References	Biochem Biophys Res Commun. 1988 Jun 30;153(3):1201-8; Am J Physiol Heart Circ Physiol. 2008 Jul;295(1):H314-26; Mol Biol Rep. 2011 Feb;38(2):905-12.