Size | Price | Stock | Qty |
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10g |
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25g |
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50g |
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100g |
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Other Sizes |
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Eprazinone diHCl, the dihydrochloride salt of Eprazinone, is a novel and potent neurokinin 1 receptor (NK1R) ligand with mucolytic, secretolytic, and bronchialantispasmodic activities.
Targets |
NK1
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ln Vitro |
Eprazinone binding to the NK1R is specifically displace. Etrimidine's mucolytic activity may be aided by NK1R blockade, despite the fact that it exhibits a relatively weak inhibition of [125I]BH-SP binding to NK1R at a concentration of 25 μM and an antagonistic effect of roughly 30%[2].
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ln Vivo |
Eprazinone (50-200 mg/kg; oral gavage; daily; for 4 days; adult male rats) at 200 mg/kg, total and individual phospholipid levels (except for phosphatidylinositol) are significantly increased, while total neutral lipid levels are decreased. Eprazinone at lower doses dramatically reduces neutral lipid levels without changing phospholipid levels[1]. The addition of eprazinone to the mucosa in studies on airway epithelial cells results in a dose-dependent, partially reversible reduction in short-circuit current (Isc). When Eprazinone concentrations are higher, both sodium and chloride transport are impacted, but at lower concentrations, the decline in Isc is solely due to a decrease in net chloride secretion[1].
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Animal Protocol |
Adult male pathogen free Fischer 344 inbred rats (200-250 g)
50 mg/kg, 100 mg/kg, and 200 mg/kg Oral gavage; daily; for 4 days |
References |
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Molecular Formula |
C₂₄H₃₄CL₂N₂O₂
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Molecular Weight |
453.44
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Exact Mass |
452.2
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Elemental Analysis |
C, 63.57; H, 7.56; Cl, 15.64; N, 6.18; O, 7.06
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CAS # |
10402-53-6
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Related CAS # |
10402-53-6 (HCl); 10402-90-1
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Appearance |
Solid powder
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SMILES |
CCOC(CN1CCN(CC1)CC(C)C(=O)C2=CC=CC=C2)C3=CC=CC=C3.Cl.Cl
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InChi Key |
BPMQVOKMMQFZGV-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C24H32N2O2.2ClH/c1-3-28-23(21-10-6-4-7-11-21)19-26-16-14-25(15-17-26)18-20(2)24(27)22-12-8-5-9-13-22;;/h4-13,20,23H,3,14-19H2,1-2H3;2*1H
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Chemical Name |
3-[4-(2-ethoxy-2-phenylethyl)piperazin-1-yl]-2-methyl-1-phenylpropan-1-one;dihydrochloride
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Synonyms |
Eprazinone diHCl
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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) |
DMSO: 1~6.3 mg/mL (2.2~13.8 mM)
Water: 18 mg/mL |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (13.78 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. Solubility in Formulation 2: ≥ 0.62 mg/mL (1.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.2 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.62 mg/mL (1.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2054 mL | 11.0268 mL | 22.0536 mL | |
5 mM | 0.4411 mL | 2.2054 mL | 4.4107 mL | |
10 mM | 0.2205 mL | 1.1027 mL | 2.2054 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.