您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > Eprazinone dihydrochloride
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Eprazinone dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Eprazinone dihydrochloride图片
CAS NO:10402-53-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
50mg电议
100mg电议
250mg电议
500mg电议
1 g电议
5 g电议

产品名称
盐酸依普拉酮
产品介绍
Eprazinone dihydrochloride 是一种具有粘液溶解,分泌分解,镇咳和支气管解痉性质的药物。Eprazinone dihydrochloride 是一种神经激肽 1 受体 (NK1R) 的配体。Eprazinone dihydrochloride 可用于慢性支气管炎的研究,可改善肺功能和动脉血氧分压。
生物活性

Eprazinone dihydrochloride is a gent with mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties. Eprazinone dihydrochloride is aneurokinin 1 receptor (NK1R)ligand. Eprazinone dihydrochloride has the potential for chronic bronchitis treatment that improved pulmonary function and arterial partial pressure of oxygen[1][2].

IC50& Target

Neurokinin 1 receptor[1]

体外研究
(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].

体内研究
(In Vivo)

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].

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

性状

Solid

Formula

C24H34Cl2N2O2

CAS 号

10402-53-6

中文名称

盐酸依普拉酮

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
In Vitro: 

H2O : ≥ 25 mg/mL(55.13 mM)

DMSO : 6.25 mg/mL(13.78 mM;ultrasonic and warming and heat to 60℃)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.2054 mL11.0268 mL22.0536 mL
5 mM0.4411 mL2.2054 mL4.4107 mL
10 mM0.2205 mL1.1027 mL2.2054 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 6.25 mg/mL (13.78 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (13.78 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

  • 2.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 0.62 mg/mL (1.37 mM); Clear solution

    此方案可获得 ≥ 0.62 mg/mL (1.37 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 6.2 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 0.62 mg/mL (1.37 mM); Clear solution

    此方案可获得 ≥ 0.62 mg/mL (1.37 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 6.2 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。