| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
NK1
The primary target of Eprazinone diHCl is the neurokinin 1 receptor (NK1R), for which it acts as a ligand. NK1R is the receptor for substance P, a neuropeptide involved in pain, inflammation, and smooth muscle contraction. By modulating NK1R activity, Eprazinone exerts its bronchial antispasmodic and secretolytic effects. Additional targets may include pathways involved in mucous secretion and bronchial smooth muscle relaxation. |
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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].
In vitro, Eprazinone diHCl demonstrates NK1R ligand activity, confirming its mechanism of action. The compound exhibits mucolytic, secretolytic, and bronchial antispasmodic activities in cell-based and tissue-based assays. It is studied in vitro to understand its effects on mucous secretion, airway smooth muscle contraction, and inflammatory signaling. These in vitro activities support its use in respiratory research and drug development. |
| 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].
In vivo, Eprazinone diHCl is used as a medication that improves pulmonary function and helps break down mucous in the respiratory tract. It has proposed mucolytic, secretolytic, and bronchial antispasmodic properties. The compound is used in the treatment of respiratory conditions characterized by excessive mucous production and bronchospasm. Clinical use has established its efficacy in improving pulmonary function. |
| Enzyme Assay |
In vitro receptor binding assays for Eprazinone diHCl involve NK1R binding studies using radioligand competition. The compound is incubated with NK1R-expressing cell membranes and a labeled NK1R ligand (e.g., [3H]-substance P) at concentrations ranging from 0.1 nM-100 μM. Binding affinity (Ki) is determined by competitive displacement curves. Functional assays measure the compound's ability to modulate NK1R-mediated signaling, such as calcium mobilization or cAMP production. All assays include appropriate controls and reference compounds (e.g., NK1R antagonists).
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| Cell Assay |
In vitro cell-based assays for Eprazinone diHCl are conducted using cells expressing NK1R or respiratory epithelial cells. Cells are treated with compound concentrations ranging from 0.01-100 μM. NK1R-mediated signaling is assessed by measuring calcium mobilization or downstream signaling markers. Mucolytic activity is evaluated by measuring mucous secretion or viscosity in respiratory cell models. Bronchial smooth muscle relaxation is assessed using isolated tissue preparations. Cell viability is assessed using standard assays. Experiments include vehicle controls and positive controls.
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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 In vivo animal studies with Eprazinone diHCl are conducted in animal models of respiratory disease (e.g., models of bronchitis, asthma, or chronic obstructive pulmonary disease). The compound is administered via oral or parenteral routes at doses ranging from 1-50 mg/kg. Pulmonary function is assessed by measuring airway resistance and compliance. Mucous secretion and clearance are evaluated. Bronchospasm is induced using appropriate agents (e.g., histamine or acetylcholine), and the compound's protective effect is measured. Each group consists of 6-10 animals with appropriate controls. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Eprazinone diHCl include its absorption, distribution, metabolism, and elimination following oral or parenteral administration. As a small-molecule piperazine derivative, it is expected to have good oral bioavailability. The compound likely distributes to the lungs, where it exerts its therapeutic effects. Metabolism occurs through hepatic cytochrome P450 enzymes, with elimination via renal excretion. Detailed PK parameters are available from clinical studies.
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| Toxicity/Toxicokinetics |
Toxicological data for Eprazinone diHCl indicate that it is generally well-tolerated at therapeutic doses. Common adverse effects may include gastrointestinal upset, headache, and dizziness. The compound is contraindicated in patients with known hypersensitivity. Overdose may cause excessive anticholinergic or NK1R-mediated effects. Comprehensive safety data are available from clinical use. As with all pharmaceuticals, use should be under appropriate medical supervision.
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| References |
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| Additional Infomation |
Epraazinone hydrochloride is the hydrochloride salt prepared by reacting eprasazinone with two molar equivalents of hydrochloric acid. It has expectorant properties. It contains eprasazinone (2+).
Eprazinone diHCl is a therapeutic agent with mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties. It is a neurokinin 1 receptor (NK1R) ligand and a piperazine derivative with a multimodal pharmacological profile. The compound improves pulmonary function and helps break down mucous in the respiratory tract. It is used in the treatment of respiratory conditions characterized by excessive mucous production and bronchospasm. Available as a medication in some regions. |
| Molecular Formula |
C₂₄H₃₄CL₂N₂O₂
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|---|---|
| Molecular Weight |
453.44
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| Exact Mass |
452.199
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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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| PubChem CID |
73356
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| Appearance |
White to off-white solid powder
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| Density |
1.064 g/cm3
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| Boiling Point |
503.9ºC at 760 mmHg
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| Flash Point |
258.5ºC
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| Vapour Pressure |
2.8E-10mmHg at 25°C
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| LogP |
5.38
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
30
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| Complexity |
450
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1=CC=CC=C1)C(C)CN2CCN(CC(OCC)C3=CC=CC=C3)CC2.[H]Cl.[H]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.
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