Art. -Nr.: HY-B0725A

Doxepin

Name: Doxepin
Brand: MedChemExpress
SKU: HY-B0725A
Price: 35.00 USD
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Rating: 5 (7 reviews)

7 Cited Publications

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Based on 7 publication(s) in Google Scholar

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

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Reinheit: 99.66%
CAS. Nr.: 1668-19-5
Formel: C₁₉H₂₁NO
Molecular Weight:279.38

Speicherung:

Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Doxepin Chemical Structure

CAS. Nr.: 1668-19-5

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (7)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Akt

mTOR

Alle Akt Isoform-spezifische Produkte anzeigen :

Alle mTOR Isoform-spezifische Produkte anzeigen :

In Vitro

Doxepin exerts protective effects by upregulating the expression of PSD-95 and synapsin 1 through activating the PI3K/AKT/mTOR signaling pathway^[1].
Doxepin 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) 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 (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 (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 (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 (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 (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 (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.

Chemical Information

CAS. Nr. 1668-19-5
Appearance < 25°C Solid, > 25°C Liquid
Molecular Weight 279.38
Formel C₁₉H₂₁NO
Color Off-white to light yellow
SMILES

CN(C)CC/C=C1C2=CC=CC=C2OCC3=CC=CC=C/13
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (357.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

3.5794 mL

17.8968 mL

35.7935 mL

5 mM

0.7159 mL

3.5794 mL

7.1587 mL

10 mM

0.3579 mL

1.7897 mL

3.5794 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 (8.95 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 (8.95 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 (8.95 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.

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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (296 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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)

Verweise

[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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.5794 mL	17.8968 mL	35.7935 mL	89.4839 mL
	5 mM	0.7159 mL	3.5794 mL	7.1587 mL	17.8968 mL
	10 mM	0.3579 mL	1.7897 mL	3.5794 mL	8.9484 mL
	15 mM	0.2386 mL	1.1931 mL	2.3862 mL	5.9656 mL
	20 mM	0.1790 mL	0.8948 mL	1.7897 mL	4.4742 mL
	25 mM	0.1432 mL	0.7159 mL	1.4317 mL	3.5794 mL
	30 mM	0.1193 mL	0.5966 mL	1.1931 mL	2.9828 mL
	40 mM	0.0895 mL	0.4474 mL	0.8948 mL	2.2371 mL
	50 mM	0.0716 mL	0.3579 mL	0.7159 mL	1.7897 mL
	60 mM	0.0597 mL	0.2983 mL	0.5966 mL	1.4914 mL
	80 mM	0.0447 mL	0.2237 mL	0.4474 mL	1.1185 mL
	100 mM	0.0358 mL	0.1790 mL	0.3579 mL	0.8948 mL

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Keywords

Doxepin

7 Cited Publications

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Doxepin

Publications Citing Use of MedChemExpress (MCE) Doxepin

Alle Akt Isoform-spezifische Produkte anzeigen

Alle mTOR Isoform-spezifische Produkte anzeigen