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| Other Sizes |
| Targets |
The primary target of S-EIT hydrobromide is inducible nitric oxide synthase (iNOS), which it inhibits. iNOS is an enzyme that produces nitric oxide (NO) from L-arginine, and its inhibition has therapeutic potential in inflammatory conditions, sepsis, and other diseases. The compound also induces the erasure of genomic imprints with a potency of 6309.6 nM and inhibits several enzymes. It produces a dose-dependent and >95% inhibition of LPS-induced increases in plasma NOx, confirming its potent iNOS inhibitory activity in vivo.
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| ln Vitro |
Type II NOS is selectively inhibited by EIT (S-ethylisothiourea) hydrobromide, which also produced a dose-dependent and >95% inhibition of LPS-induced increases in plasma [NOx]. EIT has an ED50 value of 0.4 mg/kg. Without altering type II NOS-dependent NO production, pretreatment with L-arginine (but not D-arginine) reduced mortality, indicating that toxicity might be caused by inhibition of other NOS subtypes (endothelial or neuronal) One [1]. Shear stress-induced fetal lung vasodilation is attenuated but not blocked by a selective NOS II antagonist. During shear stress-induced pulmonary vasodilation, stimulation of NOS II activity (perhaps from smooth muscle cells) partly contributes to the NO-mediated decrease in PVR (pulmonary vascular resistance). More INOS were produced by spleenocytes stimulated with alloantigens in the presence of AMT or S-ethylisothiourea (EIT), a selective iNOS inhibitor, than by cells stimulated in the absence of iNOS inhibitors. IL-10 and interleukin (IL)-4. IFN-γ and IL-2, two Th1 cytokines, were not produced more when NO synthesis was inhibited. Acute injection of EIT (380 nmol/h), an additional selective inhibitor of inducible nitric oxide synthase, also reduced the increases in effective renal plasma flow and glomerular filtration rate that are caused by pregnancy.
In vitro, S-EIT hydrobromide is used as a biochemical reagent and as an iNOS inhibitor. It induces the erasure of genomic imprints with a potency of 6309.6 nM and inhibits several enzymes. It produces a dose-dependent inhibition of LPS-induced increases in NO production in cell-based assays. Cellular assays typically evaluate its effects on NO production, iNOS activity, and downstream signaling pathways. The compound's ability to inhibit iNOS makes it valuable for studying inflammation and related conditions. |
| ln Vivo |
In vivo, S-EIT hydrobromide produces a dose-dependent and >95% inhibition of LPS-induced increases in plasma [NOx], demonstrating its potent iNOS inhibitory activity in animal models. The compound's inhibition of iNOS has potential therapeutic applications in inflammatory conditions, sepsis, and other diseases. The compound is classified for research use only and is not intended for human or veterinary therapeutic applications. Specific in vivo data for therapeutic applications is limited, though its effects on NO production have been documented.
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| Enzyme Assay |
In vitro enzyme assays for S-EIT hydrobromide typically evaluate its activity as an iNOS inhibitor. A standard assay protocol involves incubating the compound with purified iNOS enzyme in appropriate buffer systems containing L-arginine and cofactors (NADPH, FAD, FMN, BH4). The compound is dissolved in DMSO or water and diluted to working concentrations. Enzyme activity is measured by quantifying NO production using the Griess reaction or by measuring the conversion of radiolabeled arginine to citrulline. IC₅₀ values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays for S-EIT hydrobromide typically evaluate its effects on NO production and iNOS activity. A standard protocol involves culturing macrophages (e.g., RAW 264.7) or other appropriate cell lines in growth medium at 37°C with 5% CO₂. Cells are stimulated with LPS to induce iNOS expression and treated with varying concentrations of the compound. NO production is measured in the culture media using the Griess reaction. iNOS protein expression is assessed by Western blot. Cell viability is assessed using MTT or similar assays. IC₅₀ values are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for S-EIT hydrobromide typically evaluate its effects on NO production and inflammation. A standard protocol involves administering the compound to rodents via intraperitoneal or intravenous injection at doses determined from preliminary studies. Animals are challenged with LPS to induce systemic inflammation. Plasma NOx levels are measured using the Griess reaction. Inflammatory markers and organ histopathology are evaluated. The compound's ability to inhibit iNOS and reduce NO production is assessed. Dosing and administration protocols depend on the specific research objectives.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for S-EIT hydrobromide is limited, as it is primarily a research reagent. The compound has a molecular weight of 185.09 g/mol and a molecular formula of C₃H₉BrN₂S. It appears as a white to yellow solid powder and is stored in a dry, cool place. As an isothiourea derivative, it may undergo metabolic oxidation and conjugation. The compound is soluble in water and organic solvents. Specific ADME data is not available.
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| Toxicity/Toxicokinetics |
S-EIT hydrobromide is classified for research use only and is not intended for human or veterinary applications. Standard safety precautions include handling with appropriate personal protective equipment (gloves, lab coat, safety goggles) in a well-ventilated area. The compound should be stored in a dry, cool place away from incompatible materials. Acute toxicity data is not readily available in the public literature. As with all research chemicals, appropriate laboratory safety practices should be followed. No specific LD₅₀ values or detailed toxicological profiles are available in the public domain.
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| Additional Infomation |
S-EIT hydrobromide (S-Ethylisothiourea hydrobromide, EIT hydrobromide, CAS 1071-37-0) is a biochemical reagent with the molecular formula C₃H₉BrN₂S. It is an iNOS inhibitor that induces the erasure of genomic imprints and inhibits several enzymes. The compound produces a dose-dependent and >95% inhibition of LPS-induced increases in plasma NOx. It is classified as a research-use-only compound not intended for diagnostic or therapeutic purposes. It is available from multiple commercial suppliers.
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| Molecular Formula |
C3H9BRN2S
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|---|---|
| Molecular Weight |
185.09
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| Exact Mass |
183.966
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| CAS # |
1071-37-0
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| Related CAS # |
2986-20-1 (Parent)
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| PubChem CID |
200213
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| Appearance |
White to yellow solid powder
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| Density |
1.19 g/cm3
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| Boiling Point |
159.6ºC at 760 mmHg
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| Melting Point |
79-81°C
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| Flash Point |
50.3ºC
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| Vapour Pressure |
2.26mmHg at 25°C
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| Index of Refraction |
1.548
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| LogP |
2.391
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
7
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| Complexity |
52.8
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Br[H].S(/C(=N\[H])/N([H])[H])C([H])([H])C([H])([H])[H]
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| InChi Key |
SWXXKWPYNMZFTE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C3H8N2S.BrH/c1-2-6-3(4)5;/h2H2,1H3,(H3,4,5);1H
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| Chemical Name |
ethyl carbamimidothioate;hydrobromide
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| HS Tariff Code |
2934.99.9001
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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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.4028 mL | 27.0139 mL | 54.0278 mL | |
| 5 mM | 1.0806 mL | 5.4028 mL | 10.8056 mL | |
| 10 mM | 0.5403 mL | 2.7014 mL | 5.4028 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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