Eprazinone dihydrochloride

Name: Eprazinone dihydrochloride
Brand: MedChemExpress
SKU: HY-B2078A
Rating: 4.5 (0 reviews)

製品番号: HY-B2078A 純度: 99.05%: Data Sheet SDS COA 取扱説明書
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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.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Eprazinone dihydrochloride 構造式

CAS 番号 : 10402-53-6

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 38	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 38	在庫あり	Estimated Time of Arrival: December 31
Solid
50 mg	$35	在庫あり	Estimated Time of Arrival: December 31
100 mg	$55	在庫あり	Estimated Time of Arrival: December 31
250 mg	$120	在庫あり	Estimated Time of Arrival: December 31
500 mg	$210	在庫あり	Estimated Time of Arrival: December 31
1 g		お問い合わせ
5 g		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 0 publication(s) in Google Scholar

Other Forms of Eprazinone dihydrochloride:

Eprazinone お問い合わせ

Neurokinin Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

NK1R NK2R NK3R

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

NK1R

体外実験

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.

体内実験

Eprazinone (50-200 mg/kg; oral gavage; daily; for 4 days; adult male rats) at a dose of 200 mg/kg significantly increases total and individual (with the exception of phosphatidylinositol) phospholipid levels and decreases total neutral lipids. Lower doses of Eprazinone significantly decrease neutral lipid levels without affecting the phospholipids^[1].
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.

Animal Model:	Adult male pathogen free Fischer 344 inbred rats (200-250 g)^[1]
Dosage:	50 mg/kg, 100 mg/kg, and 200 mg/kg
Administration:	Oral gavage; daily; for 4 days
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.

分子量

453.44

分子式

C₂₄H₃₄Cl₂N₂O₂

CAS 番号

10402-53-6

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=CC=C1)C(C)CN2CCN(CC(OCC)C3=CC=CC=C3)CC2.Cl[H].Cl[H]

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶剤 & 溶解度

体外:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

* 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 6.25 mg/mL (13.78 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 2

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.
Protocol 3

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:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

純度とドキュメンテーション

純度: 99.05%

Select Batch:

データシート (273 KB) SDS (393 KB)

COA (247 KB) HNMR (291 KB) LCMS (105 KB)

取扱説明書 (2659 KB)

参考文献

[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

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.