Eprazinone dihydrochloride
Based on 1 Customer Validation
Eprazinone dihydrochloride is a gent with mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties. Eprazinone dihydrochloride is a neurokinin 1 receptor (NK1R) ligand. Eprazinone dihydrochloride has the potential for chronic bronchitis treatment that improved pulmonary function and arterial partial pressure of oxygen.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.05%
- CAS No.: 10402-53-6
- 화학식: C24H34Cl2N2O2
- 분자량:453.44
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
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NK1R |
In Vitro
Eprazinone specifically displaces binding to the NK1R. Although Eprazinone displays a rather weak inhibition of [125I]BH-SP binding to NK1R, at a concentration of 25 μM, and an antagonistic effect of about 30%, NK1R blockade could contribute to its mucolytic activity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
In airway epithelial studies, mucosal addition of Eprazinone produces a dose-dependent partially reversible decrease in short-circuit current (Isc). The decrease in Isc at lower Eprazinone concentrations is accounted for entirely by a decrease in net chloride secretion while at higher concentrations both sodium and chloride transport are affected[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male pathogen free Fischer 344 inbred rats (200-250 g)[1]
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Dosage:50 mg/kg, 100 mg/kg, and 200 mg/kg
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Administration:Oral gavage; daily; for 4 days
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Result:At a dose of 200 mg/kg significantly increased total and individual (with the exception of phosphatidylinositol) phospholipid levels and decreased total neutral lipids.
Chemical Information
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CAS No. 10402-53-6
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Appearance Solid
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분자량 453.44
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화학식 C24H34Cl2N2O2
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Color White to off-white
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SMILES
O=C(C1=CC=CC=C1)C(C)CN2CCN(CC(OCC)C3=CC=CC=C3)CC2.Cl[H].Cl[H]
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
In Vitro:
H2O : ≥ 25 mg/mL (55.13 mM)
DMSO : 6.25 mg/mL (13.78 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.62 mg/mL (1.37 mM); Clear solution
This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.62 mg/mL (1.37 mM); Clear solution
This protocol yields a clear solution of ≥ 0.62 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
순도&문서
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. R S Thrall, et al. Eprazinone Alters Lung Lavage Lipid Levels and Transtracheal Ion Transport. Exp Lung Res. May-Jun 1992;18(3):409-20. [Content Brief]
[2]. Yvonne Krautscheid, et al. Pharmacophore Modeling, Virtual Screening, and in Vitro Testing Reveal Haloperidol, Eprazinone, and Fenbutrazate as Neurokinin Receptors Ligands. J Chem Inf Model. 2014 Jun 23;54(6):1747-57. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.2054 mL | 11.0268 mL | 22.0536 mL | 55.1341 mL |
| 5 mM | 0.4411 mL | 2.2054 mL | 4.4107 mL | 11.0268 mL | |
| 10 mM | 0.2205 mL | 1.1027 mL | 2.2054 mL | 5.5134 mL | |
| H2O | 15 mM | 0.1470 mL | 0.7351 mL | 1.4702 mL | 3.6756 mL |
| 20 mM | 0.1103 mL | 0.5513 mL | 1.1027 mL | 2.7567 mL | |
| 25 mM | 0.0882 mL | 0.4411 mL | 0.8821 mL | 2.2054 mL | |
| 30 mM | 0.0735 mL | 0.3676 mL | 0.7351 mL | 1.8378 mL | |
| 40 mM | 0.0551 mL | 0.2757 mL | 0.5513 mL | 1.3784 mL | |
| 50 mM | 0.0441 mL | 0.2205 mL | 0.4411 mL | 1.1027 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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