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MEG hemisulfate

MEG hemisulfate (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。

CAS号

3979-00-8

分子式

C6H20N6O4S3

主要靶点

NO Synthase|NOS

仅限科研使用

Cat No : CM10949

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Synonyms

(2-巯基乙基)-胍硫酸盐|MEG|MEG Hemisulfate|Mercaptoethylguanidine|Mercaptoethylguanidine Hemisulfate|Mercaptoethylguanidine hemisulfate|iNOS



产品信息

MEG hemisulfate (Mercaptoethylguanidine hemisulfate) acts as a highly potent and selective suppressor of inducible NO synthase (iNOS), demonstrating EC50 values of 11.5 μM for iNOS, 110 μM for ecNOS, and 60 μM for bNOS in tissue homogenates. It is notably effective as a peroxynitrite scavenger and blocks peroxynitrite-triggered oxidative mechanisms. Furthermore, this compound offers protective benefits across various experimental inflammation prototypes, such as ischemia/reperfusion injury, hemorrhagic shock, periodontitis, inflammatory bowel disease, and both endotoxic and septic shock.

CAS号 3979-00-8
分子式 C6H20N6O4S3
主要靶点 NO Synthase|NOS
主要通路 免疫与炎症
分子量 336.44
纯度 99.81%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Pure form: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
别名 (2-巯基乙基)-胍硫酸盐|MEG|MEG Hemisulfate|Mercaptoethylguanidine|Mercaptoethylguanidine Hemisulfate|Mercaptoethylguanidine hemisulfate|iNOS

体内活性

MEG (30-60 mg/kg; a single i.p.) decreases mean arterial blood pressure (MAP) of normal rats[1]. 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[3]. MEG (10 mg/kg; a single i.p.) improves the renal dysfunction and tissue injury induced by ischemia/reperfusion (I/R) of rat kidney[4].

体外活性

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[1]. MEG (1 μM-3 mM; 3 min) dose-dependently inhibits the peroxynitrite-induced oxidation of cytochrome c2+ 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[2].

溶解度

DMSO:45 mg/mL (133.75 mM)

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.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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