1. Neuronal Signaling
  2. Serotonin Transporter
  3. Venlafaxine hydrochloride

Venlafaxine hydrochloride  (Synonyms: Wy 45030 hydrochloride)

Art. -Nr.: HY-B0196A Reinheit: 99.76%
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Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant.

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Venlafaxine hydrochloride

Venlafaxine hydrochloride Chemische Struktur

CAS. Nr. : 99300-78-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO Auf Lager
Solid
5 mg Auf Lager
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Based on 6 publication(s) in Google Scholar

Other Forms of Venlafaxine hydrochloride:

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Beschreibung

Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant[1].

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
2.55 3
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
0.2 3
Compound: Venlafaxine HCl
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
[PMID: 27041397]
HEK293 IC50
0.2 3
Compound: Venlafaxine HCl
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
[PMID: 27041397]
HEK293 IC50
0.2 3
Compound: Venlafaxine hydrochloride
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
[PMID: 27647372]
HEK293 IC50
0.2 3
Compound: Venlafaxine HCl
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
[PMID: 28807575]
HEK293 IC50
0.2 3
Compound: Venlafaxine hydrochloride
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
[PMID: 28274674]
HEK293 IC50
0.2 3
Compound: Venlafaxine hydrochloride
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
[PMID: 27647372]
HEK293 IC50
2.55 3
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
0.2 3
Compound: Venlafaxine hydrochloride
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
[PMID: 28274674]
HEK293 IC50
2.55 3
Compound: Venlafaxine HCl
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
0.204 3
Compound: Venlafaxine HCl
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
[PMID: 26337019]
HEK293 IC50
2.553 3
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
15700 1
Compound: venlafaxine
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
[PMID: 25221656]
HEK293 IC50
0.204 3
Compound: Venlafaxine HCl
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
[PMID: 26337019]
HEK293 IC50
2.55 3
Compound: Venlafaxine HCl
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
0.2 3
Compound: Venlafaxine HCl
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
[PMID: 28807575]
HEK293 IC50
2.55 3
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 3
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 3
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
36.1 1
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
2.55 3
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 3
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
5720 1
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]
HEK293 IC50
15700 1
Compound: venlafaxine
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
[PMID: 25221656]
HEK293 IC50
2.553 3
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 1
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 1
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]
In Vitro

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.

In Vivo

Venlafaxine hydrochloride (Wy 45030 hydrochloride; 10-100 mg/kg; IP) dose-dependently blocks the depletion of norepinephrine levels in rat hypothalamus induced by 6-OHDA[1].

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

Animal Model: Male Sprague-Dawley rats weighing 180-230 grams[1]
Dosage: 10, 30, 100 mg/kg
Administration: IP; one hour prior to p-chloramphetamine hydrochloride (p-CA; 10 mg/kg; i.p.)
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.
Molekulargewicht

313.86

Formel

C17H28ClNO2

CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

OC1(C(C2=CC=C(OC)C=C2)CN(C)C)CCCCC1.Cl

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1861 mL 15.9307 mL 31.8613 mL
5 mM 0.6372 mL 3.1861 mL 6.3723 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, 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.

  • Molaritätsrechner

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (7.97 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.
  • Protocol 2

    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.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (318.61 mM); Clear solution; Need ultrasonic

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.
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).
Reinheit & Dokumentation

Purity: 99.76%

Verweise

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.

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Produktname:
Venlafaxine hydrochloride
Art. -Nr.:
HY-B0196A
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