Doxepin Hydrochloride

Name: Doxepin Hydrochloride
Brand: MedChemExpress
SKU: HY-B0725
Rating: 5.0 (4 reviews)

Cat. No.: HY-B0725 Purity: 99.79%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.
.

For research use only. We do not sell to patients.

Doxepin Hydrochloride Chemical Structure

CAS No. : 1229-29-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
500 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
1 g	USD 60	In-stock	Estimated Time of Arrival: December 31
5 g	USD 156	In-stock	Estimated Time of Arrival: December 31
10 g	USD 192	In-stock	Estimated Time of Arrival: December 31
50 g		Get quote

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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Doxepin Hydrochloride:

Doxepin-d₃ hydrochloride Get quote
Doxepin Get quote
Doxepin Hydrochloride (Standard) Get quote

4 Publications Citing Use of MCE Doxepin Hydrochloride

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histamine Receptor Isoform Specific Products:

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H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms

CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

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.

Clinical Trial

Molecular Weight

315.84

Formula

C₁₉H₂₂ClNO

CAS No.

1229-29-4

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

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
10 mM	0.3166 mL	1.5831 mL	3.1662 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)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.92 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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)

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).

Purity & Documentation

Purity: 99.79%

Select Batch:

Data Sheet (283 KB) SDS (584 KB)

COA (255 KB) HNMR (268 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. http://pdsp.med.unc.edu/pdsp.php

[2]. Hajak, G., et al., Doxepin in the treatment of primary insomnia: a placebo-controlled, double-blind, polysomnographic study. J Clin Psychiatry, 2001. 62(6): p. 453-63. [Content Brief]

[3]. AnnemiekVermeeren, etal. Effects of the use of hypnotics on cognition. Progress in brain research vol. 190 (2011): 89-103. [Content Brief]

[4]. G Hajak, etal. Doxepin in the treatment of primary insomnia: a placebo-controlled, double-blind, polysomnographic study. The Journal of clinical psychiatry vol. 62,6 (2001): 453-63. [Content Brief]

[5]. Mahsa Gharzi, etal. Effects of different doses of doxepin on passive avoidance learning in rats. Advanced biomedical research vol. 2 66. 30 Jul. 2013. [Content Brief]

[6]. Jimei Bu, etal. Mechanism underlying the effects of doxepin on β-amyloid -induced memory impairment in rats. Iran J Basic Med Sci. 2017 Sep;20(9):1044-1049. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	3.1662 mL	15.8308 mL	31.6616 mL	79.1540 mL
	5 mM	0.6332 mL	3.1662 mL	6.3323 mL	15.8308 mL
	10 mM	0.3166 mL	1.5831 mL	3.1662 mL	7.9154 mL
	15 mM	0.2111 mL	1.0554 mL	2.1108 mL	5.2769 mL
	20 mM	0.1583 mL	0.7915 mL	1.5831 mL	3.9577 mL
	25 mM	0.1266 mL	0.6332 mL	1.2665 mL	3.1662 mL
	30 mM	0.1055 mL	0.5277 mL	1.0554 mL	2.6385 mL
	40 mM	0.0792 mL	0.3958 mL	0.7915 mL	1.9789 mL
	50 mM	0.0633 mL	0.3166 mL	0.6332 mL	1.5831 mL
	60 mM	0.0528 mL	0.2638 mL	0.5277 mL	1.3192 mL
	80 mM	0.0396 mL	0.1979 mL	0.3958 mL	0.9894 mL
	100 mM	0.0317 mL	0.1583 mL	0.3166 mL	0.7915 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.