MEG (sulfate)
(Synonyms: Mercaptoethylguanidine hemisulfate) 目录号 : GC13380A selective iNOS inhibitor and scavenger of peroxynitrite
Cas No.:3979-00-8
Sample solution is provided at 25 µL, 10mM.
MEG is a selective inhibitor of the inducible NO synthase (iNOS) [1].
NO synthase catalyses the oxidation of the amino acid L-arginine to citrulline and NO. Low concentrations of NO stimulate guanylate cyclase activity and trigger the formation of cyclic GMP (cGMP), an important messenger mediating physiological functions of NO such as vascular homeostasis. At higher concentrations, NO produced by iNOS interact with thiol groups or transition-metalcontaining proteins and can alter protein function or initiate gene expression to protect cells [2].
In vitro: In tissue homogenates, the EC50 values of MEG for inhibition of iNOS (LPS-treated rat lung), eNOS (bovine endothelial), and nNOS (rat brain) were 11.5, 110, and 60 μM, respectively [1]. MEG reduced nitrite/nitrate concentrations in the exudate and the activity of the inducible isoform of NO synthase in the lung ex vivo. In the inflamed tissues, MEG reduced the appearance of nitrotyrosine immunoreactivity [3].
In vivo: Mercaptoethylguanidine (MEG) slightly decreased the mean arterial blood pressure (MAP) in control rats. In endotoxin-treated rats, MEG increased MAP and restored 80% of the endotoxin-induced fall in MAP [1]. High doses of MEG (30–60 mg/kg) decreased MAP in normal rats [1]. In two models of acute inflammation, when given at 25 μg/paw in the paw edema model and 10 mg/kg in the pleurisy model, MEG inhibited the inflammatory response [3].
References:
[1] Southan G J, Zingarelli B, O'Connor M, et al. Spontaneous rearrangement of aminoalkylisothioureas into mercaptoalkylguanidines, a novel class of nitric oxide synthase inhibitors with selectivity towards the inducible isoform[J]. British journal of pharmacology, 1996, 117(4): 619-632.
[2] Beck K F, Eberhardt W, Frank S, et al. Inducible NO synthase: role in cellular signalling[J]. Journal of Experimental Biology, 1999, 202(6): 645-653.
[3] Cuzzocrea S, Zingarelli B, Hake P, et al. Antiinflammatory effects of mercaptoethylguanidine, a combined inhibitor of nitric oxide synthase and peroxynitrite scavenger, in carrageenan-induced models of inflammation[J]. Free Radical Biology and Medicine, 1998, 24(3): 450-459.
Cas No. | 3979-00-8 | SDF | |
别名 | Mercaptoethylguanidine hemisulfate | ||
化学名 | (2-mercaptoethyl)-guanidine sulfate | ||
Canonical SMILES | N/C(N([H])CCS)=N/[H].O=S(O)(O)=O | ||
分子式 | [C3H9N3S]2 · H2SO4 | 分子量 | 336.4 |
溶解度 | ≤10mg/ml in PBS(pH7.2) | 储存条件 | Store at 4°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.9727 mL | 14.8633 mL | 29.7265 mL |
5 mM | 0.5945 mL | 2.9727 mL | 5.9453 mL |
10 mM | 0.2973 mL | 1.4863 mL | 2.9727 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
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