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N1,n4-二(buta-2,3-二enyl)丁烷-1,4-二胺双盐酸盐

用途

MDL 72527二盐酸盐是一种有效的多胺氧化酶(PAO)抑制剂。MDL 72527二盐酸盐显示出溶酶体运动作用。MDL 72527二盐酸盐显示出神经保护作用[1][2]。

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名称

[ CAS 号 ]:
93565-01-6

[ 中文名 ]:
N1,n4-二(buta-2,3-二enyl)丁烷-1,4-二胺双盐酸盐

[ 英文名 ]:
MDL 72527

[英文别名 ]:

生物活性

[ 描述 ]:

MDL 72527二盐酸盐是一种有效的多胺氧化酶(PAO)抑制剂。MDL 72527二盐酸盐显示出溶酶体运动作用。MDL 72527二盐酸盐显示出神经保护作用[1][2]。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 神经疾病

[ 靶点 ]

polyamine oxidase (PAO)[1]

[体外研究]

MDL 72527二盐酸盐(300µM；24小时)在 M14重量细胞中出现明显的形态学变化,出现大量溶酶体和大量细胞质空泡[2]。细胞毒性试验[2]细胞系：M14细胞浓度：300µM培养时间：24小时结果：对黑色素瘤细胞的细胞存活没有显著影响。

[体内研究]

MDL 72527二盐酸盐(100 mg/kg；腹腔注射；一次)对暂时性局灶性脑缺血后的神经元细胞损伤具有神经保护作用[1]。动物模型：250-300 g,雄性自发性高血压大鼠(SHR)[1]剂量：100 mg/kg给药：I.p。；结果：平均动脉血压显著降低,皮层脑水肿形成率从85.7±0.3变为84.5±0.9%,皮层下水肿形成率由79.9±1.7变为78.4±2.0%(差异不显著),皮层和皮层下缺血损伤体积分别减少22%和17%。

[参考文献]

[1]. Doğan A, et al. Effects of MDL 72527, a specific inhibitor of polyamine oxidase, on brain edema, ischemic injury volume, and tissue polyamine levels in rats after temporary middle cerebral artery occlusion. J Neurochem. 1999 Feb;72(2):765-70.

[2]. Agostinelli E, et al. Toxicity of enzymatic oxidation products of spermine to human melanoma cells (M14): sensitization by heat and MDL 72527. Biochim Biophys Acta. 2006 Oct;1763(10):1040-50.

物理化学性质

[ 沸点 ]:
300.7ºC at 760mmHg

[ 分子式 ]:
C₁₂H₂₂Cl₂N₂

[ 分子量 ]:
265.22200

[ 闪点 ]:
159.2ºC

[ 精确质量 ]:
264.11600

[ PSA ]:
24.06000

[ LogP ]:
4.01380

[ 折射率 ]:
1.536

[ 储存条件 ]:
2-8°C

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

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

[ 海关编码 ]:
2921290000

海关

[ 海关编码 ]: 2921290000

[ 中文概述 ]:
2921290000. 其他无环多胺及其衍生物及它们的盐. 增值税率:17.0%. 退税率:9.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2921290000 other acyclic polyamines and their derivatives; salts thereof。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。MFN tariff:6.5%。General tariff:30.0%

文献

How important is the oxidative degradation of spermine?: minireview article.

Amino Acids 26(4) , 317-9, (2004)

Spermine is a constituent of most eucaryotic cells, however, it is not of vital importance for the vertebrate organism, as is demonstrated by the existence of transgenic (Gy) mice that lack spermine a...

Polyamine metabolism is involved in adipogenesis of 3T3-L1 cells.

Amino Acids 42(2-3) , 619-26, (2012)

Polyamines spermidine and spermine are known to be required for mammalian cell proliferation and for embryonic development. Alpha-difluoromethylornithine (DFMO), an inhibitor of ornithine decarboxylas...

Synergism between apple procyanidins and lysosomotropic drugs: potential in chemoprevention.

Anticancer Res. 26(5A) , 3381-5, (2006)

Procyanidins are apple constituents with potential in colon cancer chemoprevention.Human colon cancer derived metastatic cells (SW620), growing under standardized conditions, were exposed to procyanid...

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