S-ethyl N-[4-(trifluoromethyl)phenyl] Isothiourea (hydrochloride) (Synonyms: EPIT) |
| Catalog No.GC10851 |
selective, competitive inhibitor of nNOS
Products are for research use only. Not for human use. We do not sell to patients.
![S-ethyl N-[4-(trifluoromethyl)phenyl] Isothiourea (hydrochloride) Chemical Structure](/media/struct/GC1/GC10851.png "S-ethyl N-[4-(trifluoromethyl)phenyl] Isothiourea (hydrochloride) Chemical Structure")
Cas No.: 163490-78-6
Sample solution is provided at 25 µL, 10mM.
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S-ethyl N-[4-(trifluoromethyl)phenyl] Isothiourea (hydrochloride) is a selective and competitive nNOS inhibitor with Ki value of 0.32 μM for the purified human enzyme [1].
Nitric oxide (NO) is an endogenously produced inorganic free radical gas which has been implicated in blood pressure homeostasis, platelet aggregation, neurotransmission, and immunological defense mechanisms. NO is synthesized by three isoforms of nitric oxide synthase (NOS): nNOS, eNOS and iNOS [1].
S-ethyl N-[4-(trifluoromethyl)phenyl] Isothiourea (hydrochloride) (EPIT) is a selective and competitive nNOS inhibitor. S-ethyl N-[4-(trifluoromethyl)phenyl] Isothiourea inhibited human nNOS, eNOS and iNOS with Ki values of 0.32 μM, 9.4 μM and 37 μM, respectively. EPIT exhibited 115-fold and 29-fold selectivity for nNOS compared to iNOS and eNOS, respectively [1].
In mice, EPIT administered intravenously at 25 mg/kg readily penetrated the blood-brain barrier, immediately reaching concentrations in the brain equal to the plasma concentration. In rat brain slices, EPIT failed to inhibit nNOS activity, possibly due to reduced intracellular uptake [1].
Reference:
[1]. Shearer BG, Lee S, Oplinger JA, et al. Substituted N-phenylisothioureas: potent inhibitors of human nitric oxide synthase with neuronal isoform selectivity. J Med Chem. 1997 Jun 6;40(12):1901-5.
| Cas No. | 163490-78-6 | SDF | |
| Synonymes | EPIT | ||
| Chemical Name | ethyl[4-(trifluoromethyl)phenyl] carbamimidothioate, hydrochloride | ||
| Canonical SMILES | CCS/C(N([H])C1=CC=C(C(F)(F)F)C=C1)=N\[H].Cl | ||
| Formula | C10H11F3N2S • HCl | M.Wt | 284.7 |
| Solubility | ≤34mg/ml in ethanol;34mg/ml in DMSO;34mg/ml in dimethyl formamide;50mg/ml in Water | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.5125 mL | 17.5623 mL | 35.1247 mL |
| 5 mM | 0.7025 mL | 3.5125 mL | 7.0249 mL |
| 10 mM | 0.3512 mL | 1.7562 mL | 3.5125 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)
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