|2-甲基-2-异硫脲半硫酸盐|CsnPharm

CAS No.: 867-44-7

S-Methylisothiourea sulfate/S-甲基异硫脲半硫酸盐 Catalog No. CSN22638

Synonyms: S-methyl Isothiourea (hemisulfate);SMIT;2-Methyl-2-thiopseudourea hemisulfate

(S)-Methylisothiourea Sulfate is a highly selective, potent and competitive inhibitor of iNOS.

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技术信息

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.5923 mL
- 17.9615 mL
- 35.9230 mL
- 5 mM
- 0.7185 mL
- 3.5923 mL
- 7.1846 mL
- 10 mM
- 0.3592 mL
- 1.7961 mL
- 3.5923 mL

技术信息

CAS号

867-44-7

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C4H14N4O4S3

运输

蓝冰

分子量

278.37

别名

S-methyl Isothiourea (hemisulfate);SMIT;2-Methyl-2-thiopseudourea hemisulfate;S-甲基异硫脲半硫酸盐

溶解度

DMSO	Insoluble
Water	25.0 mg/mL (89.8 mM)
Ethanol	Insoluble

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S-Methylisothiourea sulfate/S-甲基异硫脲半硫酸盐 Catalog No. CSN22638

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