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钙蛋白酶抑制剂III

钙蛋白酶抑制剂III用途

MDL-28170 (Calpain Inhibitor III) 是一种有效的、选择性的、具有膜渗透性的半胱氨酸蛋白酶 (calpain)抑制剂,可在全身给药后迅速穿过血脑屏障。MDL-28170 还能阻断γ-secretase。

钙蛋白酶抑制剂III名称

[ CAS 号 ]:
88191-84-8

[ 中文名 ]:
钙蛋白酶抑制剂III

[ 英文名 ]:
Calpain Inhibitor III

[中文别名 ]:

抑制剂/苯基异丙酮胺基-N-苯甲酸甲酯

[英文别名 ]:

CARBOBEZOXY-VALINYL-PHENYLALANINALZ-VAL-PHE-CHO
MFCD00798796
N-benzyloxycarbonyl-(S)-valinylphenylalaninal
benzyl [(2S)-1-oxo-3-phenylpropan-2-yl]carbamate
Z-Val-Phe-H
Z-VAL-PHE-CHO
(S)-(-)-2-(Benzylcarbonylamino)-3-phenylpropanal
Z-L-Val-L-Phe-OH
Benzyl [(2S)-1-oxo-3-phenyl-2-propanyl]carbamate
CARBOBENZOXY-VALINYL-PHENYLALANINAL

钙蛋白酶抑制剂III生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 蛋白酶体

研究领域 >> 炎症/免疫

研究领域 >> 神经疾病

[ 靶点 ]

Calpain[1].

[体外研究]

MDL-28170显着和时间依赖性地改善海马切片中延长的中度缺氧后没有缺氧去极化的突触反应的恢复[1]。 MDL-28170剂量依赖性地抑制脑半胱氨酸蛋白酶活性(体外Ki =0.01μM)[2]。

[体内研究]

用MDL-28170(50mg/kg,ip)治疗完全防止两个治疗组中的每一个中的四只动物的纹状体损伤。在分别在0.5和3小时再循环时开始MDL-28170注射的动物中,坏死神经元的数量减少了85％和68％[2]。 MDL-28170(30 mg/kg,ip)可降低液体叩诊损伤后胼call体的功能和结构恶化[3]。 MDL-28170(10mg/kg,ip)显着改善糖尿病大鼠的神经功能参数。 MDL-28170(3和10 mg/kg,ip)可改善糖尿病大鼠的伤害性行为[5]。

[参考文献]

[1]. Chen ZF, et al. Neuronal recovery after moderate hypoxia is improved by the calpain inhibitor MDL28170. Brain Res. 1997 Sep 19;769(1):188-92.

[2]. Li PA, et al. Postischemic treatment with calpain inhibitor MDL 28170 ameliorates brain damage in a gerbil model of global ischemia. Neurosci Lett. 1998 May 8;247(1):17-20.

[3]. Ai J, et al. Calpain inhibitor MDL-28170 reduces the functional and structural deterioration of corpus callosum following fluid percussion injury. J Neurotrauma. 2007 Jun;24(6):960-78.

[4]. De Strooper B, et al. A presenilin-1-dependent gamma-secretase-like protease mediates release of Notch intracellular domain. Nature. 1999 Apr 8;398(6727):518-22.

[5]. Kharatmal SB, et al. Calpain inhibitor, MDL 28170 confer electrophysiological, nociceptive and biochemical improvement in diabetic neuropathy. Neuropharmacology. 2015 Oct;97:113-21.

[相关活性小分子]

钙蛋白酶抑制剂III物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
450.4±45.0 °C at 760 mmHg

[ 分子式 ]:
C₂₂H₂₆N₂O₄

[ 分子量 ]:
382.45

[ 闪点 ]:
226.2±28.7 °C

[ PSA ]:
84.50000

[ LogP ]:
3.77

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.571

[ 储存条件 ]:
2-8℃

钙蛋白酶抑制剂IIIMSDS

详细MSDS(安全技术说明书)

钙蛋白酶抑制剂III安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
22-24/25

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

钙蛋白酶抑制剂III文献

Impaired Focal Adhesion Kinase-Grb2 Interaction during Elevated Activity in Hippocampal Neurons.

Int. J. Mol. Sci. 16 , 15659-69, (2015)

Excitatory/inhibitory imbalances are implicated in many neurological disorders. Previously, we showed that chronically elevated network activity induces vulnerability in neurons due to loss of signal ...

A recoverable state of axon injury persists for hours after spinal cord contusion in vivo.

Nat. Commun. 5 , 5683, (2014)

Therapeutic strategies for spinal cord injury (SCI) commonly focus on regenerating disconnected axons. An alternative approach would be to maintain continuity of damaged axons, especially after contus...

Different patterns of electrical activity lead to long-term potentiation by activating different intracellular pathways.

J. Neurosci. 35(2) , 621-33, (2015)

Deciphering and storing information coded in different firing patterns are important properties of neuronal networks, as they allow organisms to respond and adapt to external and internal events. Here...

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