★【medlife】(S)-Methylisothiourea sulfate.
iNOS抑制剂，S-甲基异硫脲硫酸盐是制备胍类的中间体，可用于制备杀菌剂二甲嘧酚、乙嘧酚，杀虫剂嘧啶氧磷、抗蚜威等 胍乙啶硫酸盐、氢化泼尼松磷酸钠的中间体 用作医药及农药中间体
中文名称
(S)-Methylisothiourea sulfate.
中文别名
S-甲基异硫脲硫酸盐;2-甲基-2-硫代异尿素硫酸氢盐;2-甲基-2-硫代假脲半硫酸盐;2-甲基-2-疏基硫酸脲;2-甲基-2-异硫脲半硫酸盐;O-甲基异脲硫酸盐;S-甲基异硫脲 半硫酸盐;硫酸S-甲基硫脲;2-甲基-2-硫代异尿素硫酸盐;2-甲基异硫脲硫酸盐;JS-甲基异硫脲硫酸盐;S-甲基-ITU;S-甲基异硫脲;甲基异硫脲硫酸盐;S-甲基硫代异尿素硫酸氢盐;2-甲基-2-硫代假脲 半硫酸盐
英文名称
Carbamimidothioic acid, methyl ester
英文别名
2-Methyl-2-thiopseudourea hemisulfate;S-Methylisothiourea sulphate;2-Methyl-2-thiopseudourea sulphate;S-Methylisothiourea hemisulfate salt;S-Methylisothiouronium sulphate;s-Methyl-Iso-Thiourea;S-EIT hemihydrate;S-Methylisothiouronium sulfate;(S)-Methylisothiourea sulfate;2-METHYL-2-THIOPSEUDOUREA HEMISULFATE HEMIHYDRATE;2-Methyl-2-thiopseudourea sulfate;2-METHYL-ISOTHIOUREA;METHYL IMIDOTHIOCARBAMATE SULFATE;S-methyl Isothiourea (hemisulfate);S-Methylisothiourea Sulfate;S-Methyl-isothiouron;S-Methyl-isothiouronium Hemisulfate;S-METHYLTHIOUREA SULFATE;methyl imidothiocarbamate;S-methyl-2-thiopseudourea hydrogen sulfate;S-Methylisothiourea hemisulfate;S-METHYLISOTHIOUREA HEMISULFATE SALT _X000D_;S-methylisothiourea hydrogensulfate;S-METHYL-ISO-THIOUREA SULFATE;S-METHYLTHIOURONIUM SULFATE FOR SYNTHESIS;SMT;Bis(2-methylthiouronium) sulphate;Bis(2-methylisothiouronium) sulphate;S-Methyl isothiourea sulfate;s-methylisothiourea;methyl carbamimidothioate;S-Methyl isothiourea;Carbamimidothioic acid, methyl ester;2-methylisothiourea;S-Methyl-isothiourea;S-Methylisothiouronium;2-methyl-2-thiopseudourea;S-Methylisothiopseudouronium;S-Methylthiopseudouronium iodide;ES8C3884JW;SDDKIZNHOCEXTF-UHFFFAOYSA-N;S-Methyl-ITU;2-Methylisothio urea;S-methylthiopseudourea;S-methylpseudothiourea;PubChem2004;S-methylthiourea;PubChem
Cas No.
867-44-7
分子式
C4N4O4S3H14
分子量
278.37
包装储存
4°C, sealed storage, away from moisture
生物活性
S-Methylisothiourea sulfate is a potent, selective and competitive inhibitor of inducible nitric oxide synthase (iNOS). S-Methylisothiourea sulfate exerts beneficial effects in rodent models of septic shock.
性状
Solid
IC50 & Target[1][2]
iNOS
体外研究(In Vitro)
S-Methylisothiourea sulfate is a competitive inhibitor of iNOS activity at the L-arginine site.
S-Methylisothiourea sulfate prevents the NO-mediated cytotoxic effect of LPS in cultured macrophages.
S-Methylisothiourea sulfate (100 nM-100 μM) exhibits inhibitory effects on LPS (ug/mL)-induced nitrite production in J774.2 macrophages and rat aortic vascular smooth muscle cells.
S-Methylisothiourea sulfate (up to 1 mM) does not inhibit the activity of xanthine oxidase, diaphorase, lactate dehydrogenase, monoamine oxidase, catalase, cytochrome P450, or superoxide dismutase.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
S-Methylisothiourea sulfate (0.01-3 mg/kg; i.v.) dose-dependently reverses the hypotension and the vascular hyporeactivity to vasoconstrictor agents caused by endotoxin LPS in anesthetized rats.
S-Methylisothiourea sulfate (5 mg/kg; i.p.; given 2 hr after LPS; 10 mg/kg; i.p.) attenuates the rises in plasma alanine and aspartate aminotransferases, bilirubin, and creatinine and also prevents hypocalcaemia when measured 6 hr after administration of LPS.
S-Methylisothiourea sulfate (1 mg/kg; i.p.) improves 24-hr survival of mice treated with a high dose of LPS (60 mg/kg; i.p.).
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Male Wistar rats (260-320 g)
Dosage: 0.01 mg/kg, 0.1 mg/kg, 1 mg/kg, 3 mg/kg
Administration: Intravenous injection
Result: Caused a prompt restoration of the blood pressure to pre-LPS levels at 3 mg/kg dose in LPS (10 mg/kg, i.v.)-treated rats; Inhibited iNOS activity measured in homogenates of lung.
运输条件
Room temperature or refrigerated transportation.
储存方式
4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. C Szabó, et al. Beneficial effects and improved survival in rodent models of septic shock with S-methylisothiourea sulfate, a potent and selective inhibitor of inducible nitric oxide synthase. Proc Natl Acad Sci U S A. 1994 Dec 20; 91(26): 12472-12476. [Information]
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