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3979-00-8

中文名稱 (2-MERCAPTOETHYL)-GUANIDINE SULFATE
CAS 3979-00-8
分子式 C3H11N3O4S2
分子量 217.267
MOL 文件 3979-00-8.mol
3979-00-8 結構式 3979-00-8 結構式

基本信息

中文別名
(2-巰基乙基)-胍硫酸鹽
英文別名
MEG SULFATE
meg hemisulfate salt
XJKZAAUVINNNNC-UHFFFAOYSA-N
(2-MERCAPTOETHYL)-GUANIDINE SULFATE
1-?(2-?Mercaptoethyl)?guanidine Sulfate
mercaptoethylguanidine hemisulfate salt

物理化學性質

熔點177-178 °C
儲存條件2-8°C

安全數(shù)據(jù)

WGK Germany3

常見問題列表

生物活性
MEG (Mercaptoethylguanidine) hemisulfate 是一種有效和選擇性的誘導型 NO 合酶 (iNOS) 的抑制劑,在組織勻漿中抑制 iNOS,ecNOS 和 bNOS 的 EC50 值分別為 11.5,110 和 60 μM。MEG hemisulfate 也有效的過氧亞硝酸鹽清除劑,可抑制過氧亞硝酸鹽誘導的氧化過程。MEG hemisulfate 在許多炎癥實驗模型中具有保護作用,包括缺血/再灌注損傷,牙周炎,失血性休克,炎性腸病以及內毒素和敗血性休克。
靶點

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

體外研究

MEG (0.1-1000 μM; 18 h) reduces nitrite accumulation in the supernatant of cultured J774.2 macrophages activated with LPS (10 μg/mL) and INF (50 μg/mL). MEG inhibits iNOS activity in homogenates of lungs taken from LPS-treated rats.
MEG (1 μM-3 mM; 3 min) dose-dependently inhibits the peroxynitrite-induced oxidation of cytochrome c 2+ and hydroxylation of benzoate.
MEG (1-300 μM) inhibits the suppression of mitochondrial respiration and DNA single strand breakage in response to peroxynitrite in J774 cells.
MEG (300 μM; 30 min) inhibits the suppression of vascular contractility in response to peroxynitrite in thoracic aortic rings.

體內研究

MEG (10 mg/kg; i.p. for 5 d) attenuates the degree of lipid peroxidation, protein oxidation, and peroxynitrites level and ameliorated the decrease of antioxidant enzymes activities in the esophagus of rats subjected to caustic burn injury.
MEG (30-60 mg/kg; a single i.p.) decreases mean arterial blood pressure (MAP) of normal rats.
MEG (10 mg/kg; a single i.p.) improves the renal dysfunction and tissue injury induced by ischemia/reperfusion (I/R) of rat kidney.

Animal Model: Sprague-Dawley rats (200-250 g) were injured the esophagus
Dosage: 10 mg/kg
Administration: I.p. for 5 days
Result: Reduced the stenosis index (SI) and the histopathologic damage score.
Decreased the malondialdehyde and protein carbonyl content and increased the activities of superoxide dismutase and glutathione peroxidase.
Regulated the nitrate and nitrite level.
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