Calpeptin 是一种具有细胞穿透性的calpain抑制剂,也是CAThepsin K 抑制剂,其对人血小板 Calpain I 的ID50值为40 nM。
产品描述
Calpeptin is a potent, cell-permeable calpain inhibitor.
体外活性
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]
体内活性
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]
Cas No.
117591-20-5
分子式
C20H30N2O4
分子量
362.47
储存和溶解度
Ethanol:67 mg/mL (184.8 mM)
DMSO:67 mg/mL (184.8 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years