Cat. No.: HY-B0725

Doxepin Hydrochloride

Name: Doxepin Hydrochloride
Brand: MedChemExpress
SKU: HY-B0725
Price: 35.00 USD
Availability: InStock
Rating: 5 (7 reviews)

7 Cited Publications

Customer Review

Based on 7 publication(s) in Google Scholar

Doxepin Hydrochloride is an orally active, blood-brain barrier penetrant tricyclic antidepressant with multiple activities including hypnosis, sedation, analgesia and vasodilation. Doxepin Hydrochloride enhances the expression of PSD-95 and synapsin 1 via the PI3K/AKT/mTOR signaling pathway, and is metabolized to DesmethylDoxepin Hydrochloride in vivo. Doxepin Hydrochloride can be used in research related to various diseases such as depression, anxiety, obesity and atopic dermatitis.

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

Purity: 99.64%
CAS No.: 1229-29-4
Formula: C₁₉H₂₂ClNO
Molecular Weight:315.84

Storage:

4°C, sealed storage, away from moisture

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

Doxepin Hydrochloride Chemical Structure

CAS No.: 1229-29-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (7)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Akt

mTOR

All Akt Isoforms :

All mTOR Isoforms :

In Vitro

Doxepin Hydrochloride exerts protective effects by upregulating the expression of PSD-95 and synapsin 1 through activating the PI3K/AKT/mTOR signaling pathway^[1].
Doxepin Hydrochloride is almost ineffective in inhibiting serotonin (5-HT) uptake in rat platelets^[2].

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

In Vivo

Doxepin (5 mg/kg; p.o.; once daily; for 56 consecutive days) Hydrochloride exacerbates obesity, glucose intolerance, non-alcoholic fatty liver disease, renal impairment, and urinary chromium loss in high-fat diet-induced obese C57BL/6J mice. This conclusion is supported by the findings of increased body weight, elevated fatty liver scores, increased blood urea nitrogen levels, enhanced urinary chromium excretion, as well as reduced insulin sensitivity and decreased renal antioxidant enzyme activity^[3].
Doxepin Hydrochloride (4.65-24.00 mg/kg; intraperitoneal injection; single administration; 5-120 minutes before electroshock) exerts dose- and time-dependent anticonvulsant activity against maximal electroshock-induced seizures in mice, with the peak efficacy observed at 5 minutes after intraperitoneal administration and an ED₅₀ of 6.6 mg/kg^[4].
Doxepin Hydrochloride (6.70-11.63 mg/kg; i.p.; single administration; 5 minutes prior to Isoniazid (HY-B0329) challenge) exhibits anticonvulsant activity against isoniazid-induced seizures in Mus musculus mice, with an ED₅₀ of 8.8 mg/kg and a protective index of 3.0^[4].
Doxepin Hydrochloride (3.88-8.04 mg/kg; intraperitoneal injection; single administration; 5 minutes prior to 3-mercaptopropionic acid challenge) exhibits anticonvulsant activity against 3-mercaptopropionic acid-induced seizures in mice, with an ED₅₀ of 5.1 mg/kg and a protective index of 5.2^[4].
Doxepin Hydrochloride (4.65-8.04 mg/kg; i.p.; single administration; 5 min prior to Bicuculline (HY-N0219) challenge) exhibits anticonvulsant activity against Bicuculline-induced seizures in mice, with an ED₅₀ of 5.9 mg/kg and a protective index of 4.5^[4].
Doxepin Hydrochloride (3.23-5.58 mg/kg; i.p.; single administration; 5 min prior to thiosemicarbazide challenge) exhibits the strongest anticonvulsant activity against thiosemicarbazide-induced seizures in mice, with an ED₅₀ of 4.3 mg/kg and a protective index of 6.1^[4].
Doxepin Hydrochloride (24.11-72.00 mg/kg; intraperitoneal injection; single administration; 5-120 minutes before rotarod test) induces time-dependent neurotoxicity in mice by impairing motor coordination, with toxicity peaking at 5 minutes after intraperitoneal administration and a TD₅₀ of 26.4 mg/kg^[4].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1229-29-4
Appearance Solid
Molecular Weight 315.84
Formula C₁₉H₂₂ClNO
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)

Publications (7)

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Journal Impact Factor

Nat Commun

Maprotiline restores ER homeostasis and rescues neurodegeneration via Histamine Receptor H1 inhibition in retinal ganglion cells. [Abstract]

2022 Nov 10;13(1):6796. PMID: 36357388
Cell Commun Signal

Tricyclic antidepressants induce liver inflammation by targeting NLRP3 inflammasome activation. [Abstract]

2023 May 25;21(1):123. PMID: 37231437
Int J Pharm

Raman-assessed cutaneous pharmacokinetics of doxepin topical products. [Abstract]

2026 Feb 18:126680. PMID: 41720364
Antiviral Res

Repurposed doxepin targeting host AXL kinase to disrupt viral 2C-mediated immune evasion in Coxsackievirus B infection. [Abstract]

2025 Dec:244:106307. PMID: 41197812
Pharm Res

Investigation of the Binding Characteristics of Agonists and Various Antagonists Targeting Histamine 1 Receptor. [Abstract]

2025 Aug;42(8):1315-1329. PMID: 40760405
Virus Res

In-vitro antiviral activity of doxepin hydrochloride against group B coxsackievirus. [Abstract]

2022 Aug:317:198816. PMID: 35598772
J Appl Toxicol

Inhibitory interaction of flavonoids with organic cation transporter 2 and their structure-activity relationships for predicting nephroprotective effects. [Abstract]

2023 Oct;43(10):1421-1435. PMID: 37057715

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

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.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Working solution concentration: 0.22 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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (303 KB)
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Bu J. 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]

[2]. Pinder R M, et al. Doxepin Up-to-Date: A Review of its Pharmacological Properties and Therapeutic Efficacy with Particular Reference to Depression. Drugs, 1977, 13: 161-218.

[3]. Chang GR, et al. Doxepin Exacerbates Renal Damage, Glucose Intolerance, Nonalcoholic Fatty Liver Disease, and Urinary Chromium Loss in Obese Mice. Pharmaceuticals (Basel, Switzerland). 2021 Mar 16;14(3):267.

[4]. Sun XY, et al. Characterization of the anticonvulsant activity of doxepin in various experimental seizure models in mice. Pharmacological reports : PR. 2009;61(2):245-51.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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.

Bioz

Keywords

Doxepin Hydrochloride

7 Cited Publications

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