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> Doxepin (Hydrochloride) [1229-29-4]

Doxepin (Hydrochloride) [1229-29-4]

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Referencia HY-B0725-500mg

embalaje : 500mg

Marca : MedChemExpress

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Descripciòn

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[1][2]. Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant[3].
. Doxepin has therapeutic effects in atopic dermatitis，chronic urticarial，can improve cognitive processes， protect central nervous system[4].
. Doxepin has also been proposed as a protective factor against oxidative stress[5].
.

IC50 & Target

H1 Receptor

 

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[6].
.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Doxepin Hydrochloride Related Antibodies

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.
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[6].
.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SD male rats[6].
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.
Ensayo clínico
Peso molecular

315.84

Fòrmula

C19H22ClNO
No. CAS
Appearance

Solid

Color

White to off-white

SMILES

CN(C)CC/C=C1C2=CC=CC=C2OCC3=CC=CC=C/13.Cl
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, sealed storage, away from moisture

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

Solvente y solubilidad
In Vitro: 

DMSO : ≥ 100 mg/mL (316.62 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 50 mg/mL (158.31 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
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.

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    40% PEG300    5% Tween-80    45% Saline

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).
Pureza y Documentación
Referencias