CAS NO: | 117591-20-5 |
规格: | ≥98% |
包装 | 价格(元) |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 362.46 |
---|---|
Formula | C20H30N2O4 |
CAS No. | 117591-20-5 |
Storage | -20℃ for 3 years in powder form |
-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 |
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. |