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CAS No.: 117591-20-5

Calpeptin/钙肽素 Catalog No. CSN10530

Synonyms: Benzylcarbonyl-leu-nleu-H;N-Cbz-leu-nleu-al

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.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Calpain is a Ca²⁺-mediated cytosolic cyctein protease existed in various cells. Calpeptin is a potent calpain inhibitor with ID₅₀ values of 52 nM, 34 nM, 138 nM, and 40 nM for Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papain, and Calpain I (human platelets), respectively. In platelets stimulated by A₂₃₁₈₇, 66% of ABP and 69% of P235 remained undegraded in the presence of 10μg/mL calpeptin, in comparison to 26% of ABP and 40% of P235 remained without calpeptin. The activity of intrinsic calpain in platelets was completely abolished by the treatment of 100μg/mL calpeptin^[4]. Calpeptin at the concentration of 34nM reduced calpain activity by 44% in the homogenate of proliferating PC12 cells. When PCI2 cells were incubated with NGF and 36μM calpeptin for 17h, the probabilities for a PCI2 cell to extend a given maximal neurite length were increased as compared to non-calpeptin-treated cells^[5]. In a murine model of middle cerebral artery occlusion, the intra-cerebroventricle injection of calpeptin (50μg dissolved in 5μL DMSO) before the occlusion resulted in a significant reduction of neuronal apoptosis in hippocampal CA1 sector, as compared to DMSO-treated animals, via the inhibition of caspase-3 expression^[6].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
COS7 cells	50 μM	Function assay	24 h	Induction of autophagy in african green monkey COS7 cells assessed as increase in autophagosome at 50 uM after 24 hrs by electron microscopy	18391949
HeLa cells	50 μM	Function assay	-	Induction of autophagy in human HeLa cells expressing EGFP-LC3 assessed as increase in LC3-2 level at 50 uM in presence of 400 nM bafilomycin A1	18391949
PC12 cells	10 μM	Function assay	96 h	Induction of autophagy in undifferentiated rat stable inducible PC12 cells expressing A53T alpha-synuclein assessed as A53T alpha-synuclein clearance at 10 uM after 96 hrs by calpain activation assay	18391949

动物研究
剂量
Mice: 10 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 10 mg/kg^[3] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7589 mL
- 13.7945 mL
- 27.5890 mL
- 5 mM
- 0.5518 mL
- 2.7589 mL
- 5.5178 mL
- 10 mM
- 0.2759 mL
- 1.3795 mL
- 2.7589 mL

技术信息

CAS号

117591-20-5

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H30N2O4

运输

蓝冰

分子量

362.46

别名

Benzylcarbonyl-leu-nleu-H;N-Cbz-leu-nleu-al

溶解度

DMSO	71.0 mg/mL (195.9 mM)
Water	Insoluble
Ethanol	72.0 mg/mL (198.6 mM)

动物实验配方

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Calpeptin/钙肽素 Catalog No. CSN10530

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