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Doxepin (hydrochloride). (Synonyms: 盐酸多塞平)
目录号: PC14686 纯度: ≥98%
CAS No. :1229-29-4
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中文名称
Doxepin (hydrochloride).
中文别名
盐酸多虑平;盐酸多塞平;N,N-二甲基-3-二苯并[b,e]-噁庚英-11(6H)亚基-丙胺盐酸盐;多虑平盐酸盐;多塞平盐酸盐;Doxepin Hydrochloride 多塞平盐酸盐;Doxepinhydrochloride(顺+反);多虑平;多虑平 盐酸盐 (异构体混合物);盐酸多虑平(Doxepin Hydrochloride )杂质对照品;盐酸多虑平(盐酸多塞平);盐酸多塞平 BP 93;盐酸多塞平 EP标准品;盐酸多塞平 USP标准品;盐酸多塞平 标准品;盐酸多塞平(异构体混合物);盐酸多塞平,对照品;11-(3-二甲基氨基亚丙基)-6,11-二氢二苯并[b,e]氧杂卓盐酸盐;N,N-二甲基-3-二苯并[B,E]-庚英-11(6H)亚基-丙胺盐酸盐;盐酸多噻平;11-(3-二甲基氨基亚丙基)-6,11-二氢二苯并[b,e]氧杂卓盐酸盐 (异构体混合物)
英文名称
Doxepin Hydrochloride
英文别名
doxepin HCL;3-(6,11-dihydrodibenz(b,e)oxepin-11-ylidene)propyldimethylamine hcl;doxepin hydrochloride;11-(3-dimethylaminopropylidene)-6,11-dihydro-benz[b,e]oxepin hcl;Doxepin Hydrochloride (mixture of isomers);Doxepin (hydrochloride);Doxepin hydrochloride solution;11-(3-Dimethylaminopropylidene)-6,11-dihydrodibenz[b,e]oxepine hydrochloride;11-(3-Dimethylaminopropylidene)-6,11-dihydrodibenzo[b,e]oxepine Hydrochloride;11-(3-Dimethylaminopropylidene)-6,11-dihydrodibenzo[b,e]oxepine Hydrochloride (mixture of isomers);11-(3-Dimethylaminopropylidene)-6,11-dihydro-benz[b,e]Oxepin;Novoxapin;Aponal;Silenor;Toruan;Curatin;Zonalon;Adapin;Doxepine hydrochloride;Novoxapin hydrochloride;MF 10 HCl;Quitaxon;Sinequan;C19H21NO.HCl;MLS000069794;CU61C5RH24;SMR000058230;Sinequan (TN);1-Propanamine, 3-dibenz(b,e)oxepin-1
Cas No.
1229-29-4
分子式
C19NOClH22
分子量
315.84
包装储存

Sealed and stored at 4℃,, away from moisture

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

生物活性

Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2. Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant.
. Doxepin has therapeutic effects in atopic dermatitis,chronic urticarial,can improve cognitive processes, protect central nervous system.
. Doxepin has also been proposed as a protective factor against oxidative stress.
.

性状

Solid

体外研究(In Vitro)

The protective effect of doxepin is associated with the enhancement of PSD-95 and synapsin 1 expression via PI3K/AKT/mTOR signaling pathway.
.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line: SH-SY5Y human neuroblastoma cell line
Concentration: 10 ng/ml
Incubation Time: 2 h
Result: Improved the protein expre-ssion levels of PSD-95, synapsin 1 and p-AKT in SH-SY5Y cells, and decreased the protein expression level of p-mTOR in SH-SY5Y cells.
体内研究(In Vivo)

Doxepin (intraperitoneal injection of 1 mg/kg and 5 mg/kg doxepin once a day for 21 days) can protect against the Aβ1-42-induced memory impairment in rats.
.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SD male rats.
Dosage: 1, 5mg/kg
Administration: Doxepin (intraperitoneal injection of 1 mg/kg and 5 mg/kg doxepin once a day for 21 days)
Result: Improved the protein expression levels of PSD-95 and synapsin 1 in hippocampus and tem-poral lobe, and decreased the protein expression level of p-AKT in hippocampus and temporal lobe after treatment of 1 mg/kg of doxepin.
运输条件

Room temperature or refrigerated transportation.

储存方式

Sealed and stored at 4℃,, away from moisture

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

ClinicalTrial
参考文献
溶解度数据
体外研究: 

DMSO : ≥ 100 mg/mL (316.62 mM)

H2O : ≥ 50 mg/mL (158.31 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1662 mL 15.8308 mL 31.6616 mL
5 mM 0.6332 mL 3.1662 mL 6.3323 mL
10 mM 0.3166 mL 1.5831 mL 3.1662 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

    建议依照次序添加每种溶剂: PBS

    Solubility: 140 mg/mL (443.26 mM); Clear solution; Need ultrasonic

  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.92 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.92 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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 ddH?O 中,得到澄清透明的生理盐水溶液
  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.92 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.92 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 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
  • 4.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.92 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.92 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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