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CALPEPTIN

CALPEPTIN用途

Calpeptin 是一种有效的、具有细胞穿透性的 calpain 抑制剂,其对人血小板 Calpain I 的ID50 值为40 nM。Calpeptin 也是cathepsin K 的抑制剂。

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CALPEPTIN名称

[ CAS 号 ]:
117591-20-5

[ 中文名 ]:
CALPEPTIN

[ 英文名 ]:
calpeptin

[英文别名 ]:

Z-LEU-NLE-CHO
BENZYLOXYCARBONYLLEUCYL-NORLEUCINAL
MFCD00155623
N-CBZ-L-LEUCYL-NORLEUCINAL
Z-Leu-Nle-H
CalpeptinN-Benzyloxycarbonyl-L-leucyl-norleucinal
CALPEPTIN
Z-LEU-NLE-OH
Z-LEU-NORLEUCINAL
N-BENZYLOXYCARBONYL-L-LEUCYLNORLEUCINAL

CALPEPTIN生物活性

[ 描述 ]:

Calpeptin 是一种有效的、具有细胞穿透性的 calpain 抑制剂,其对人血小板 Calpain I 的ID50 值为40 nM。Calpeptin 也是cathepsin K 的抑制剂。

[ 相关类别 ]:

研究领域 >> 炎症/免疫

信号通路 >> 代谢酶/蛋白酶 >> 蛋白酶体

信号通路 >> 代谢酶/蛋白酶 >> 组织蛋白酶

[ 靶点 ]

ID50: 40 nM (Calpain I in human platelets)[1]. Cthepsin K[2]

[体外研究]

Calpeptin(0-100nM,24小时)处理以剂量依赖性方式抑制WI38 VA13和IMR90细胞的增殖。 Calpeptin(1000 pg/ml,24小时)抑制IL-6诱导的肺成纤维细胞增殖[3]。细胞增殖测定[3]细胞系：WI38 VA13和IMR90细胞浓度：0-100nM孵育时间：24小时结果：以剂量依赖性方式抑制增殖。

[体内研究]

含有Bleo的Calpeptin(0.04 mg /小鼠,腹腔注射,每周3次,28天)给药可显着抑制博来霉素治疗的小鼠肺组织中胶原沉积和钙蛋白酶活性的增加[3]。动物模型：C57BL/6雌性小鼠(8周龄)[3]。剂量：0.04毫克/小鼠。给药：每周腹腔注射三次,共28天(与Bleo一起)。结果：抑制了博来霉素处理的小鼠肺组织中胶原沉积和钙蛋白酶活性的增加。

[参考文献]

[1]. Tsujinaka T, et al. Synthesis of a new cell penetrating calpain inhibitor (calpeptin). Biochem Biophys Res Commun. 1988 Jun 30;153(3):1201-8.

[2]. Catalano JG, et al. Design of small molecule ketoamide-based inhibitors of cathepsin K. Bioorg Med Chem Lett. 2004 Feb 9;14(3):719-22.

[3]. Tabata C, et al. The calpain inhibitor calpeptin prevents pulmonary fibrosis in mice. Clin Exp Immunol. 2010 Dec;162(3):560-7.

CALPEPTIN物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
550.7±45.0 °C at 760 mmHg

[ 熔点 ]:
60-75 °C

[ 分子式 ]:
C₂₀H₃₀N₂O₄

[ 分子量 ]:
362.463

[ 闪点 ]:
286.8±28.7 °C

[ 精确质量 ]:
362.220551

[ PSA ]:
84.50000

[ LogP ]:
4.37

[ 外观性状 ]:
白色至灰白色粉末

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.508

[ 储存条件 ]:
-20°C

CALPEPTINMSDS

CALPEPTIN安全信息

[ 安全声明 (欧洲) ]:
S24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

CALPEPTIN合成路线

CALPEPTIN上下游产品

CALPEPTIN上游产品

CALPEPTIN下游产品

CALPEPTIN文献

Calpain mediates processing of the translation termination factor eRF3 into the IAP-binding isoform p-eRF3.

FEBS Lett. 589 , 2241-7, (2015)

The involvement of polypeptide chain-releasing factor eRF3 in translation termination and mRNA decay is well established. Moreover, the finding that the proteolytically processed isoform of eRF3 (p-eR...

Cytosolic HMGB1 controls the cellular autophagy/apoptosis checkpoint during inflammation.

J. Clin. Invest. 125(3) , 1098-110, (2015)

The intracellular protein HMGB1 is released from cells and acts as a damage-associated molecular pattern molecule during many diseases, including inflammatory bowel disease (IBD); however, the intrace...

Salbutamol inhibits RhoA activation in normal but not in desensitized bronchial smooth muscle cells.

J. Pharm. Pharmacol. 67 , 1416-20, (2015)

This study was aimed at investigating whether the β2 -adrenoceptor agonist, salbutamol, could modulate RhoA activation in normal and homologously desensitized bronchial smooth muscle cells (BSMC).Seru...

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