| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg | ||
| Other Sizes |
| Targets |
iNOS
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|---|---|
| ln Vitro |
S-methylisothiourea sulfate is an inhibitor of iNOS activity at the L-arginine site that is competitive [1]. On cultured macrophages, S-methylisothiourea sulfate inhibits the NO-mediated cytotoxicity of LPS [1]. In J774.2 macrophages and rat aorta vascular smooth muscle cells, LPS (μg/mL)-induced nitrite generation is inhibited by S-methylisothiourea sulfate (100 nM-100 μM) [1].The activities of xanthine oxidase, diaphorase, lactate dehydrogenase, monoamine oxidase, catalase, cytochrome P450, and superoxide dismutase are not inhibited by S-methylisothiourea sulfate (up to 1 mM) [1].
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| ln Vivo |
In anesthetized rats, S-Methylisothiourea suLfate (0.01-3 mg/kg; i.v.) dose-dependently reverses endotoxin LPS-induced hypotension and vascular hyporesponsiveness to vasoconstrictors [1]. When assessed six hours after the injection of lipopolysaccharide (LPS), S-methylisothiourea sulfate (5 mg/kg; i.p.; given 2 hours after LPS; 10 mg/kg; i.p.) attenuates plasma alanine and aspartate aminotransferases, bilirubin, and elevations in creatinine. It also provides protection against hypocalcemia [1]. Mice treated with high-dose LPS (60 mg/kg; i.p.) have a higher 24-hour survival rate when given S-methylisothiourea sulfate (1 mg/kg; i.p.) [1].
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| Animal Protocol |
Animal/Disease Models: Male Wistar rats (260-320 g)[1]
Doses: 0.01 mg/kg, 0.1 mg/kg, 1 mg/kg, 3 mg/kg Route of Administration: intravenous (iv)injection Experimental Results: Caused a prompt restoration of the blood pressure to pre-LPS levels at 3 mg/kg dose in LPS (10 mg/kg, iv)-treated rats; Inhibited iNOS activity measured in homogenates of lung . |
| References |
[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.
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| Molecular Formula |
C2H6N2S.1/2H2O4S
|
|---|---|
| Molecular Weight |
139.18
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| CAS # |
867-44-7
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| SMILES |
S(C([H])([H])[H])/C(=N\[H])/N([H])[H]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O : 65 mg/mL (467.02 mM)
DMSO : < 1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (359.25 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 7.1849 mL | 35.9247 mL | 71.8494 mL | |
| 5 mM | 1.4370 mL | 7.1849 mL | 14.3699 mL | |
| 10 mM | 0.7185 mL | 3.5925 mL | 7.1849 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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