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MEG (sulfate) Sale

(Synonyms: Mercaptoethylguanidine hemisulfate) 目录号 : GC13380

A selective iNOS inhibitor and scavenger of peroxynitrite

MEG (sulfate) Chemical Structure

Cas No.:3979-00-8

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5mg
¥952.00
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Sample solution is provided at 25 µL, 10mM.

Description

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.

化学性质

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
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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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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
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