Venlafaxine hydrochloride
Based on 6 publication(s) in Google Scholar
Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant.
For research use only. We do not sell to patients.
- Purity: 99.58%
- CAS No.: 99300-78-4
- Formula: C17H28ClNO2
- Molecular Weight:313.86
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Venlafaxine hydrochloride
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.2 μM
Compound: Venlafaxine HCl
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Inhibition of [3H]-5-HT reuptake in human SERT transfected into HEK293 cells by liquid scintillation counting method
Inhibition of [3H]-5-HT reuptake in human SERT transfected into HEK293 cells by liquid scintillation counting method
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[PMID: 27041397] |
| HEK293 | IC50 |
0.2 μM
Compound: Venlafaxine HCl
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Inhibition of re-uptake of [3H]-5-HT at human SERT expressed in HEK293 cells by liquid scintillation counting
Inhibition of re-uptake of [3H]-5-HT at human SERT expressed in HEK293 cells by liquid scintillation counting
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[PMID: 28807575] |
| HEK293 | IC50 |
0.2 μM
Compound: Venlafaxine hydrochloride
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Inhibition of [3H]-5-hydroxytryptamine reuptake in human SERT expressed in HEK293 cells by liquid scintillation counting method
Inhibition of [3H]-5-hydroxytryptamine reuptake in human SERT expressed in HEK293 cells by liquid scintillation counting method
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[PMID: 27647372] |
| HEK293 | IC50 |
0.2 μM
Compound: Venlafaxine hydrochloride
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Inhibition of [3H]-5-hydroxytryptamine reuptake in human SERT expressed in HEK293 cells by microbeta liquid scintillation counting method
Inhibition of [3H]-5-hydroxytryptamine reuptake in human SERT expressed in HEK293 cells by microbeta liquid scintillation counting method
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[PMID: 28274674] |
| HEK293 | IC50 |
0.204 μM
Compound: Venlafaxine HCl
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Inhibition of human SERT expressed in HEK293 cells assessed as reduction of serotonin reuptake using [3H]-SERT after 15 mins by liquid scintillation counting
Inhibition of human SERT expressed in HEK293 cells assessed as reduction of serotonin reuptake using [3H]-SERT after 15 mins by liquid scintillation counting
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[PMID: 26337019] |
| HEK293 | IC50 |
15700 nM
Compound: venlafaxine
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Inhibition of human DAT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay
Inhibition of human DAT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay
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[PMID: 25221656] |
| HEK293 | IC50 |
2.55 μM
Compound: Venlafaxine HCl
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Inhibition of [3H]-NE reuptake in human NET transfected into HEK293 cells by liquid scintillation counting method
Inhibition of [3H]-NE reuptake in human NET transfected into HEK293 cells by liquid scintillation counting method
|
[PMID: 27041397] |
| HEK293 | IC50 |
2.55 μM
Compound: Venlafaxine HCl
|
Inhibition of re-uptake of [3H]-NE at human NET expressed in HEK293 cells by liquid scintillation counting
Inhibition of re-uptake of [3H]-NE at human NET expressed in HEK293 cells by liquid scintillation counting
|
[PMID: 28807575] |
| HEK293 | IC50 |
2.55 μM
Compound: Venlafaxine hydrochloride
|
Inhibition of [3H]-5-dopamine reuptake in human DAT expressed in HEK293 cells by liquid scintillation counting method
Inhibition of [3H]-5-dopamine reuptake in human DAT expressed in HEK293 cells by liquid scintillation counting method
|
[PMID: 27647372] |
| HEK293 | IC50 |
2.55 μM
Compound: Venlafaxine hydrochloride
|
Inhibition of [3H]-5-norepinephrine reuptake in human NET expressed in HEK293 cells by liquid scintillation counting method
Inhibition of [3H]-5-norepinephrine reuptake in human NET expressed in HEK293 cells by liquid scintillation counting method
|
[PMID: 27647372] |
| HEK293 | IC50 |
2.55 μM
Compound: Venlafaxine hydrochloride
|
Inhibition of [3H]-5-norepinephrine reuptake in human NET expressed in HEK293 cells by microbeta liquid scintillation counting method
Inhibition of [3H]-5-norepinephrine reuptake in human NET expressed in HEK293 cells by microbeta liquid scintillation counting method
|
[PMID: 28274674] |
| HEK293 | IC50 |
2.553 μM
Compound: Venlafaxine HCl
|
Inhibition of human NET expressed in HEK293 cells assessed as reduction of serotonin reuptake using [3H]-NET after 15 mins by liquid scintillation counting
Inhibition of human NET expressed in HEK293 cells assessed as reduction of serotonin reuptake using [3H]-NET after 15 mins by liquid scintillation counting
|
[PMID: 26337019] |
| HEK293 | IC50 |
36.1 nM
Compound: venlafaxine
|
Inhibition of human SERT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay
Inhibition of human SERT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay
|
[PMID: 25221656] |
| HEK293 | IC50 |
5720 nM
Compound: venlafaxine
|
Inhibition of human NET expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay
Inhibition of human NET expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay
|
[PMID: 25221656] |
Venlafaxine hydrochloride (Wy 45030 hydrochloride) dose-dependently inhibits binding of the serotonin transporter radioligand [3H]-paroxetine to membranes from cells transfected with the human 5-HT transporter with a Ki of 2.48 μM. Venlafaxine hydrochloride inhibits binding of the NE transporter ligand [3H]-nisoxetine to membranes from cells transfected with the human NE transporter with a Ki of 82 nM[1].
Venlafaxine hydrochloride inhibits ex vivo binding to rat 5-HT transporters and NE transporters with ED50 values of 2 and 54 mg/kg, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats weighing 180-230 grams[1]
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Dosage:10, 30, 100 mg/kg
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Administration:IP; one hour prior to p-chloramphetamine hydrochloride (p-CA; 10 mg/kg; i.p.)
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Result:Dose-dependently blocked the depletion of norepinephrine levels in rat hypothalamus induced by 6-OHDA (intracerebroventricularly; 50 μg/rat; one hour later), with ED50 values of 12 and 94 mg/kg i.p., respectively.
Chemical Information
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CAS No. 99300-78-4
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Appearance Solid
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Molecular Weight 313.86
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Formula C17H28ClNO2
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Color White to off-white
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SMILES
OC1(C(C2=CC=C(OC)C=C2)CN(C)C)CCCCC1.Cl
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Synonyms
Wy 45030 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (6)
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Journal Impact Factor
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Most Recent
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Water Res
Enhanced venlafaxine degradation in amorphous FeS2 under redox-dynamic aqueous environments: Critical role of citrate in electron utilization for boosted hydroxyl radical generation. [Abstract]2025 Oct 1;288(Pt B):124709. PMID: 41046790 -
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J Med Chem
Exploring Simple Drug Scaffolds from the Generated Database Chemical Space Reveals a Chiral Bicyclic Azepane with Potent Neuropharmacology. [Abstract]2025 Apr 24. PMID: 40274264 -
Neurosci Bull
Targeting 5-HT to Alleviate Dose-Limiting Neurotoxicity in Nab-Paclitaxel-Based Chemotherapy. [Abstract]2025 Jul;41(7):1229-1245. PMID: 40369268 -
J Agric Food Chem
Fluoride Stimulates Anxiety- and Depression-like Behaviors Associated with SIK2-CRTC1 Signaling Dysfunction. [Abstract]2021 Nov 17;69(45):13618-13627. PMID: 34735150 -
Int Immunopharmacol
Innovative role of the antidepressant imipramine in esophageal squamous cell carcinoma treatment: Promoting apoptosis and protective autophagy. [Abstract]2025 Feb 6:147:113969. PMID: 39764996
Solvent & Solubility
H2O : ≥ 100 mg/mL (318.61 mM)
DMSO : 50 mg/mL (159.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* 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.
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.97 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.97 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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (318.61 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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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.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Bymaster FP, et al. Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors. Neuropsychopharmacology. 2001 Dec;25(6):871-80. [Content Brief]
[2]. Goeringer KE, et al. Postmortem tissue concentrations of venlafaxine. Forensic Sci Int. 2001 Sep 15;121(1-2):70-5. [Content Brief]
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 3.1861 mL | 15.9307 mL | 31.8613 mL | 79.6534 mL |
| 5 mM | 0.6372 mL | 3.1861 mL | 6.3723 mL | 15.9307 mL | |
| 10 mM | 0.3186 mL | 1.5931 mL | 3.1861 mL | 7.9653 mL | |
| 15 mM | 0.2124 mL | 1.0620 mL | 2.1241 mL | 5.3102 mL | |
| 20 mM | 0.1593 mL | 0.7965 mL | 1.5931 mL | 3.9827 mL | |
| 25 mM | 0.1274 mL | 0.6372 mL | 1.2745 mL | 3.1861 mL | |
| 30 mM | 0.1062 mL | 0.5310 mL | 1.0620 mL | 2.6551 mL | |
| 40 mM | 0.0797 mL | 0.3983 mL | 0.7965 mL | 1.9913 mL | |
| 50 mM | 0.0637 mL | 0.3186 mL | 0.6372 mL | 1.5931 mL | |
| 60 mM | 0.0531 mL | 0.2655 mL | 0.5310 mL | 1.3276 mL | |
| 80 mM | 0.0398 mL | 0.1991 mL | 0.3983 mL | 0.9957 mL | |
| 100 mM | 0.0319 mL | 0.1593 mL | 0.3186 mL | 0.7965 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.