MEG hemisulfate

MEG hemisulfate用途

MEG (Mercaptoethylguanidine) hemisulfate 是一种有效和选择性的诱导型 NO 合酶 (iNOS) 的抑制剂,在组织匀浆中抑制 iNOS,ecNOS 和 bNOS 的 EC50 值分别为 11.5,110 和 60 μM。MEG hemisulfate 也有效的过氧亚硝酸盐清除剂,可抑制过氧亚硝酸盐诱导的氧化过程。MEG hemisulfate 在许多炎症实验模型中具有保护作用,包括缺血/再灌注损伤,牙周炎,失血性休克,炎性肠病以及内毒素和败血性休克。

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MEG hemisulfate名称

[ CAS 号 ]:
3979-00-8

[ 中文名 ]:
MEG(硫酸盐)

[ 英文名 ]:
MEG hemisulfate

[英文别名 ]:

2-(2-Sulfanylethyl)guanidine sulfate (2:1)
2-(2-sulfanylethyl)guanidine,sulfuric acid
Guanidine, N''-(2-mercaptoethyl)-, sulfate (2:1)
MEG hemisulfate salt

MEG hemisulfate生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> 一氧化氮合酶

研究领域 >> 炎症/免疫

[ 靶点 ]

IC50: 11.5 μM (iNOS), 110 μM (ecNOS), 60 μM (bNOS)[1]

[体外研究]

兆欧表(0.1-1000μ米；18h)减少LPS激活的培养J774.2巨噬细胞上清中亚硝酸盐的积累(10μg/mL)和INF(50μg/mL)。MEG抑制LPS处理大鼠肺匀浆中iNOS的活性[1]。梅格(1μM-3毫米；3分钟)剂量依赖性地抑制过氧亚硝酸盐诱导的细胞色素c2+氧化和苯甲酸羟基化[2]。MEG(1-300μM) 抑制J774细胞线粒体呼吸和DNA单链断裂对过氧亚硝酸盐的反应[2]。兆欧表(300μ米；30分钟)抑制对胸主动脉环中过氧亚硝酸盐反应的血管收缩抑制[2]。

[体内研究]

MEG(10mg/kg；i、 p.5d)可减轻碱烧伤大鼠食管脂质过氧化、蛋白质氧化和过氧亚硝酸盐水平,改善抗氧化酶活性的下降[3]。MEG(30-60毫克/千克；单次腹腔注射可降低正常大鼠的平均动脉血压(MAP)[1]。MEG(10mg/kg；单次i.p.)可改善大鼠肾脏缺血/再灌注(i/R)引起的肾功能不全和组织损伤[4]。动物模型：Sprague-Dawley大鼠(200-250g)损伤食管[3]剂量：10mg/kg给药：腹腔注射,连续5d。结果：降低狭窄指数(SI)和组织病理学损伤评分。降低丙二醛和蛋白质羰基含量,提高超氧化物歧化酶和谷胱甘肽过氧化物酶活性。调节硝酸盐和亚硝酸盐水平。

[参考文献]

[1]. Southan GJ, et, al. Spontaneous rearrangement of aminoalkylisothioureas into mercaptoalkylguanidines, a novel class of nitric oxide synthase inhibitors with selectivity towards the inducible isoform. Br J Pharmacol. 1996 Feb;117(4):619-32.

[2]. Szabó C, et, al. Mercaptoethylguanidine and guanidine inhibitors of nitric-oxide synthase react with peroxynitrite and protect against peroxynitrite-induced oxidative damage. J Biol Chem. 1997 Apr 4;272(14):9030-6.

[3]. Guven A, et, al. Mercaptoethylguanidine attenuates caustic esophageal injury in rats: a role for scavenging of peroxynitrite. J Pediatr Surg. 2011 Sep;46(9):1746-52.

[4]. Guven A, et, al. Scavenging of peroxynitrite reduces renal ischemia/reperfusion injury. Ren Fail. 2008;30(7):747-54.

MEG hemisulfate物理化学性质

[ 沸点 ]:
645.7ºC at 760 mmHg

[ 分子式 ]:
C₆H₂₀N₆O₄S₃

[ 分子量 ]:
336.456

[ 闪点 ]:
344.3ºC

[ 精确质量 ]:
336.070801

[ PSA ]:
284.38000

[ LogP ]:
1.60840

[ 储存条件 ]:
2-8°C，干燥，密封

MEG hemisulfateMSDS

详细MSDS(安全技术说明书)

MEG hemisulfate安全信息

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

[ 危害码 (欧洲) ]:
Xi

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

MEG hemisulfate文献

Nitric oxide is synthesized in acute leukemia cells after exposure to phenolic antioxidants and initially protects against mitochondrial membrane depolarization.

Cancer Lett. 215(1) , 43-52, (2004)

We investigated the early events involved in loss of mitochondrial membrane potential (DeltaPsi(mt)) leading to apoptosis in cells derived from patients with acute lymphocytic leukemia after exposure ...

Mitogen-activated protein kinase phosphorylation in kidneys of beta(s) sickle cell mice.

J. Am. Soc. Nephrol. 11(6) , 1026-32, (2000)

Previous studies in beta(s) sickle cell mice demonstrated renal immunostaining for nitrotyrosine, which is putative evidence of peroxynitrite (ONOO(-)) formation. ONOO(-) is known to nitrate tyrosine ...

Inhibition of nitric oxide synthase ameliorates cellular injury in sickle cell mouse kidneys.

Kidney Int. 58(1) , 82-9, (2000)

In previous studies of transgenic sickle cell mice, increased renal expression of inducible nitric oxide synthase (iNOS) and endothelial cell isoform of NOS (EcNOS) was found by Western blot and immun...

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