Art. -Nr.: HY-B1272

Desipramine hydrochloride

15 Cited Publications

Kundenbewertung

Based on 15 publication(s) in Google Scholar

Desipramine hydrochloride is a first-generation tricyclic antidepressant. Desipramine hydrochloride selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine hydrochloride activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine hydrochloride also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine hydrochloride can be used for the research of hepatocellular cancer, inflammation, and neurological diseases.

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Reinheit: 99.76%
CAS. Nr.: 58-28-6
Formel: C₁₈H₂₃ClN₂
Molecular Weight:302.84

Speicherung:

4°C, sealed storage, away from moisture

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

Desipramine hydrochloride Chemical Structure

CAS. Nr.: 58-28-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (15)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

ERK1

ERK2

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

Alle ERK Isoform-spezifische Produkte anzeigen :

Alle JNK Isoform-spezifische Produkte anzeigen :

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

Alle AP-1 Isoform-spezifische Produkte anzeigen :

Alle TNF Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.0063 μM Compound: Desipramine	Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 174586 Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 174586	[PMID: 34112854]

In Vitro

Desipramine hydrochloride (3-500 µM; 24 h) reduces the viability of human hepatoma Hep3B cells in a dose-dependent manner^[1].
Desipramine hydrochloride (10-500 µM; 24 h) induces cytotoxicity in human hepatoma Hep3B cells in a dose-dependent manner, as measured by increased LDH release^[1].
Desipramine hydrochloride (3-100 µM; 24 h) increases intracellular ROS production in human hepatoma Hep3B cells in a dose-dependent manner^[1].
Desipramine hydrochloride (3-100 µM µM; 24 h) has its induced cell death in human hepatoma Hep3B cells abolished by the ROS scavenger NAC (HY-B0215) at concentrations up to 30 µM, and partially reduced at 100 µM after 24 h^[1].
Desipramine hydrochloride (3-100 µM; 24 h) reduces mitochondrial membrane potential in human hepatoma Hep3B cells in vitro in a dose-dependent manner^[1].
Desipramine hydrochloride (100 µM; 1-8 h) activates ERK1/2, JNK, and p38 MAPK signaling in human hepatoma Hep3B cells-^[1].
Desipramine hydrochloride (3-100 µM; 24 h) has its induced cell death in human hepatoma Hep3B cells abolished by inhibition of ERK1/2, p38, or JNK MAPK signaling^[1].
Desipramine hydrochloride (30-500 µM) increases intracellular calcium levels in human hepatoma Hep3B cells in a concentration-dependent manner, with increases occurring via both extracellular calcium influx and intracellular calcium release^[1].
Desipramine hydrochloride potently binds to the rat norepinephrine transporter with a K_i of 6.2 nM, showing 25-fold selectivity over the rat serotonin transporter (K_i = 158 nM) ^[3].
Desipramine hydrochloride (1 h) binds to the rat α₂D-adrenoceptor with a K_i of 3.4 μM^[3].
Desipramine hydrochloride potently binds to the human norepinephrine transporter with a K_i of 0.63 nM, has lower affinity for the human serotonin transporter (K_i = 22 nM), and lacks affinity for the human dopamine transporter (K_i >10,000 nM)^[3].
Desipramine hydrochloride (0.01-10 μM; 20 h) dose-dependently inhibits LPS (HY-D1056)-induced TNF-α release from primary human monocytes^[4].
Desipramine hydrochloride (10 μM) reduces TNF-α-induced RANTES release and RANTES mRNA accumulation in A549 human lung epithelial cells^[4].
Desipramine hydrochloride (10 μM) represses TNF-α-induced NF-κB activity in A549 human lung epithelial cells^[4].
Desipramine hydrochloride (10 μM) reduces TPA (HY-18739)-induced AP-1 activity in A549 human lung epithelial cells^[4].

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

Cell Viability Assay^[1]

Cell Line:

human hepatoma Hep3B cells
Concentration:

1 µM, 3 µM, 10 µM, 30 µM, 100 µM, 300 µM, 500 µM
Incubation Time:

24 h
Result:

Did not affect cell viability at 1 µM.
Reduced cell viability to 90.2% of control at 3 µM.
Reduced cell viability to 87.4% of control at 10 µM.
Reduced cell viability to 69.1% of control at 30 µM.
Reduced cell viability to 45.9% of control at 100 µM.
Reduced cell viability to 36.1% of control at 300 µM.
Reduced cell viability to 27.8% of control at 500 µM.
Caused statistically significant viability reductions at concentrations ≥3 µM compared to control.

Western Blot Analysis^[1]

Cell Line:

human hepatoma Hep3B cells
Concentration:

100 µM
Incubation Time:

1 h, 2 h, 4 h, 8 h
Result:

Increased phosphorylation of ERK1/2 to 185.2% of control at 1 h, 151.5% of control at 2 h, and 138.5% of control at 4 h.
Increased phosphorylation of p38 to 135.1% of control at 1 h and 116.4% of control at 2 h.
Increased phosphorylation of JNK to 118.9% of control at 1 h and 113.9% of control at 2 h.
Maintained unchanged total levels of ERK1/2, JNK, and p38 across all time points.
Caused statistically significant increases in MAPK phosphorylation at the specified time points compared to control.

In Vivo

Desipramine (5-20 mg/kg; i.p.; single dose, 30 minutes pre-LPS) hydrochloride dose-dependently inhibits LPS (HY-D1056)-induced serum TNF-α production and increases survival rate to 70% in a murine septic shock model^[4].
Desipramine (10 mg/kg; i.p.; daily; 8 days, 30 minutes pre-Ovalbumin nebulization) hydrochloride reduces lung inflammation by decreasing macrophage and lymphocyte counts in Ovalbumin (HY-W250978)-sensitized rats but does not attenuate bronchial hyperresponsiveness^[4].

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

Animal Model:

LPS-induced BALB/c mice (5-week-old, 17-21 g)^[4]
Dosage:

5, 10, 20 mg/kg
Administration:

i.p.; single dose (preventive, 30 minutes pre-LPS)
Result:

Significantly inhibited LPS-induced serum TNF-α production.
Increased mouse survival rate to 70% with preventive 20 mg/kg treatment (vs 10% in saline controls).

Animal Model:

Ovalbumin-sensitized Brown Norway rats (10-week-old)^[4]
Dosage:

10 mg/kg
Administration:

i.p.; daily; 8 days (30 minutes pre-ovalbumin nebulization)
Result:

Did not reduce bronchial hyperresponsiveness to metacholine (measured by enhanced pause, Penh).
Reduced total number of inflammatory cells in bronchoalveolar lavages.
Decreased macrophage count by 52% compared to saline-treated sensitized rats.
Decreased lymphocyte count by 21% compared to saline-treated sensitized rats.
Did not reduce neutrophil or eosinophil counts compared to saline-treated sensitized rats.

Clinical Trial

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

Chemical Information

CAS. Nr. 58-28-6
Appearance Solid
Molecular Weight 302.84
Formel C₁₈H₂₃ClN₂
Color White to off-white
SMILES

CNCCCN1C2=CC=CC=C2CCC3=CC=CC=C31.Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

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

Publications (15)

All Bio/Physico-chemical AssayCell Proliferation/Viability AssayWBCell Imaging/Staining

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Journal Impact Factor

Cell

Unveiling conformation-selective regulation of the norepinephrine transporter. [Abstract]

2025 Nov 26;188(24):6861-6872.e14. PMID: 41138730
Acta Pharm Sin B

2026 Jan 27.
Sci Total Environ

Cadmium exacerbates liver injury by remodeling ceramide metabolism: Multiomics and laboratory evidence. [Abstract]

2024 May 1:923:171405. PMID: 38432385

Desipramine hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Total Environ. 2024 May 1:923:171405. [Abstract]

Desipramine hydrochloride (Des; 0-50 μM; 24 h). Cell viability of BRL-3A cells after Des intervention was detected by CCK-8. Other groups were compared with 0 μM group.

Desipramine hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Total Environ. 2024 May 1:923:171405. [Abstract]

Desipramine hydrochloride (Des; 12.5 μM; 24 h). The expression levels of apoptosis-related proteins in BRL-3A cells were detected by western blotting.

Desipramine hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Total Environ. 2024 May 1:923:171405. [Abstract]

Desipramine hydrochloride (Des; 12.5 μM; 24 h). Hoechst/PI double staining: Hoechst/PI was used to double stain and observe them under fluorescence microscope (200×). Hoechst 33342 can stain the nucleus with blue fluorescence. PI can stain necrotic cells with red fluorescence.

Desipramine hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Total Environ. 2024 May 1:923:171405. [Abstract]

Desipramine hydrochloride (Des; 12.5 μM; 24 h). The level of LDH in cell culture medium after 12.5 μM Des intervention and/or 20 μM Cadmium exposure for 24 h.
Br J Pharmacol

Serotonergic transmission plays differentiated roles in the rapid and sustained antidepressant-like effects of ketamine. [Abstract]

2024 Dec;181(23):4874-4889. PMID: 39238235
J Med Chem

Bioisostere-Driven Discovery of SePP: A Selenium-Containing Polypharmacological Agent Relevant to Fragile X Syndrome. [Abstract]

2026 Feb 10. PMID: 41666325
Neural Regen Res

Glucagon-like peptide-1/glucose-dependent insulinotropic polypeptide dual receptor agonist DA-CH5 is superior to exendin-4 in protecting neurons in the 6-hydroxydopamine rat Parkinson model. [Abstract]

2021 Aug;16(8):1660-1670. PMID: 33433498
Pharmaceutics

Laminin Receptor-Mediated Nanoparticle Uptake by Tumor Cells: Interplay of Epigallocatechin Gallate and Magnetic Force at Nano-Bio Interface. [Abstract]

2022 Jul 22;14(8):1523. PMID: 35893779

Desipramine hydrochloride purchased from MedChemExpress. Usage Cited in: Pharmaceutics. 2022 Jul 22;14(8):1523. [Abstract]

Figure shows that 10 and 30 μM of Desipramine hydrochloride attenuated EGCG-induced enhancement of MNPcell by 8.9% and 39.3% in the Mag− group, respectively. In the Mag+ group, MNPcell was enhanced up to 6.6-fold by EGCG compared with the control group, which was minorly attenuated by 5.7% and 11.2% by Desipramine hydrochloride at 10 and 30 μM, respectively.
Glia

Potassium channel Kir 4.1 regulates oligodendrocyte differentiation via intracellular pH regulation. [Abstract]

2022 Nov;70(11):2093-2107. PMID: 35775976
Inflammation

Acid Sphingomyelinase and Acid β-Glucosidase 1 Exert Opposite Effects on Interleukin-1β-Induced Interleukin 6 Production in Rheumatoid Arthritis Fibroblast-Like Synoviocytes. [Abstract]

2021 Aug;44(4):1592-1606. PMID: 33665756
J Parkinson Dis

The Novel Dual GLP-1/GIP Receptor Agonist DA-CH5 Is Superior to Single GLP-1 Receptor Agonists in the MPTP Model of Parkinson's Disease. [Abstract]

2020;10(2):523-542. PMID: 31958096
Biochim Biophys Acta Mol Basis Dis

Involvement of Kir4.1 in pain insensitivity of the BTBR mouse model of autism spectrum disorder. [Abstract]

2023 Mar 28;1869(5):166700. PMID: 36990129
Neurotoxicology

Ropivacaine-induced seizures evoked pain sensitization in rats: Participation of 5-HT/5-HT3R. [Abstract]

2022 Dec:93:173-185. PMID: 36209936
Neuroscience

Acute Administration of Lactate Exerts Antidepressant-like Effect Through cAMP-dependent Protein Synthesis. [Abstract]

2024 Mar 26:542:11-20. PMID: 38336096
Parkinsons Dis

DA5-CH and Semaglutide Protect against Neurodegeneration and Reduce α-Synuclein Levels in the 6-OHDA Parkinson's Disease Rat Model. [Abstract]

2022 Nov 14:2022:1428817. PMID: 36419409
Research Square Print

2023 Feb 23.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (330.21 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 100 mg/mL (330.21 mM; Need ultrasonic)

* "≥" 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

3.3021 mL

16.5104 mL

33.0207 mL

5 mM

0.6604 mL

3.3021 mL

6.6041 mL

10 mM

0.3302 mL

1.6510 mL

3.3021 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* 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.

Molaritätsrechner

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

Mass

Konzentration

Volumen

Molecular Weight

Verdünnungsrechner

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

Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)}

Konzentration _{(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 (8.26 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 (8.26 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 (8.26 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: 1 mg/mL (3.30 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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.

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) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 KB)
SDS (419 KB)
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- Portuguese - PT (419 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]. Yang DK, et al. Desipramine induces apoptosis in hepatocellular carcinoma cells. Oncol Rep. 2017;38(2):1029-1034. [Content Brief]

[2]. Kishore-Kumar R, et al. Desipramine relieves postherpetic neuralgia. Clin Pharmacol Ther. 1990;47(3):305-312. [Content Brief]

[3]. Deupree JD, et al. Pharmacological properties of the active metabolites of the antidepressants desipramine and citalopram. Eur J Pharmacol. 2007;576(1-3):55-60. [Content Brief]

[4]. Roumestan C, et al. Anti-inflammatory properties of desipramine and fluoxetine. Respir Res. 2007;8(1):35. Published 2007 May 3. [Content Brief]

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
DMSO / H₂O	1 mM	3.3021 mL	16.5104 mL	33.0207 mL	82.5518 mL
	5 mM	0.6604 mL	3.3021 mL	6.6041 mL	16.5104 mL
	10 mM	0.3302 mL	1.6510 mL	3.3021 mL	8.2552 mL
	15 mM	0.2201 mL	1.1007 mL	2.2014 mL	5.5035 mL
	20 mM	0.1651 mL	0.8255 mL	1.6510 mL	4.1276 mL
	25 mM	0.1321 mL	0.6604 mL	1.3208 mL	3.3021 mL
	30 mM	0.1101 mL	0.5503 mL	1.1007 mL	2.7517 mL
	40 mM	0.0826 mL	0.4128 mL	0.8255 mL	2.0638 mL
	50 mM	0.0660 mL	0.3302 mL	0.6604 mL	1.6510 mL
	60 mM	0.0550 mL	0.2752 mL	0.5503 mL	1.3759 mL
	80 mM	0.0413 mL	0.2064 mL	0.4128 mL	1.0319 mL
	100 mM	0.0330 mL	0.1651 mL	0.3302 mL	0.8255 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.

Keywords

Desipramine hydrochloride

15 Cited Publications

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Desipramine hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Desipramine hydrochloride

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Alle ERK Isoform-spezifische Produkte anzeigen

Alle JNK Isoform-spezifische Produkte anzeigen

Alle p38 MAPK Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Alle AP-1 Isoform-spezifische Produkte anzeigen

Alle TNF Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (15)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation