S-Methylisothiourea sulfate

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Chemical Structure| 867-44-7 同义名 : S-甲基异硫脲硫酸盐 ;S-methyl Isothiourea (hemisulfate);(S)-Methylisothiourea sulfate;SMIT
CAS号 : 867-44-7
货号 : A258497
分子式 : C4H14N4O4S3
纯度 : 97%
分子量 : 278.373
MDL号 : MFCD00013055
存储条件：

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 65 mg/mL(233.5 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 (S)-Methylisothiourea (S-Methylisothiourea) Sulfate (SMT) is a potent, selective and competitive inhibitor of inducible nitric oxide synthase (iNOS). 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. SMT is equipotent with MeArg in inhibiting the endothelial, constitutive isoform of NOS in vitro and causes increases in blood pressure similar to those produced by MeArg in normal rats. SMT, however, dose-dependently reverses (0.01-3 mg/kg) the hypotension and the vascular hyporeactivity to vasoconstrictor agents caused by endotoxin [bacterial lipopolysaccharide (LPS), 10 mg/kg, i.v.] in anesthetized rats. Moreover, therapeutic administration of SMT (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. SMT (1 mg/kg, i.p.) improves 24-hr survival of mice treated with a high dose of LPS (60 mg/kg, i.p.)[1]. In addition, S-methylisothiourea (SMT) had anti-inflammatory effects in treating herpes simplex encephalitis in mice, and SMT also induced apoptosis of herpes simplex virus (HSV-1)-infected microglial cells[2]. SMT (30 mg/kg) attenuates the MIA-induced pain and histopathological changes in the knee joint. The antinociceptive and antiarthritic effects of SMT were mediated by inhibiting cartilage damage and suppression of NO in synovial fluid[3]. HOT (Hyperbaric oxygen treatment) and SMT together were significantly more effective in preventing weight loss and in reducing inflammation and the severity of colitis histology when compared with HOT and SMT separately[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.59mL

0.72mL

0.36mL

17.96mL

3.59mL

1.80mL

35.92mL

7.18mL

3.59mL
参考文献

[1]Szabó C, Southan GJ, Thiemermann C. 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):12472-6

[2]Guo YJ, Li W, Li XF, Zhao L, Zhang SL, Zhou Y, Dong JH, Mei YW. S-methylisothiourea induces apoptosis of herpes simplex virus-1-infected microglial cells. Inflammation. 2011 Oct;34(5):388-401

[3]More AS, Kumari RR, Gupta G, Lingaraju MC, Balaganur V, Pathak NN, Kumar D, Kumar D, Sharma AK, Tandan SK. Effect of iNOS inhibitor S-methylisothiourea in monosodium iodoacetate-induced osteoathritic pain: implication for osteoarthritis therapy. Pharmacol Biochem Behav. 2013 Feb;103(4):764-72

[4]Demirci H, Polat Z, Uygun A, Kadayifci A, Sager O, Oztutk K, Sahiner F, Caliskan B, Karslioglu Y, Ozler M, Ozel M, Ergun H, Ozturk O, Beyzadeoglu M, Bagci S. The Effect of the iNOS Inhibitor S-Methylisothiourea and Hyperbaric Oxygen Treatment on Radiation Colitis in Rats. Acta Gastroenterol Belg. 2016 Mar;79(1):8-13