(2-MERCAPTOETHYL)-GUANIDINE SULFATE
- CAS号:3979-00-8
- 英文名:(2-MERCAPTOETHYL)-GUANIDINE SULFATE
- 中文名:(2-MERCAPTOETHYL)-GUANIDINE SULFATE
- CBNumber:CB4129697
- 分子式:C3H11N3O4S2
- 分子量:217.26714
- MOL File:3979-00-8.mol
- 熔点 :177-178 °C
- 储存条件 :2-8°C
- 溶解度 :PBS (7.2): 10 mg/ml
- 形态 :A crystalline solid
- WGK Germany :3
(2-MERCAPTOETHYL)-GUANIDINE SULFATE性质、用途与生产工艺
- 生物活性 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。
-
靶点
IC50: 11.5 μM (iNOS), 110 μM (ecNOS), 60 μM (bNOS)
-
体外研究
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. -
体内研究
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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