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Venlafaxine HCl Serotonin Transporter inhibitor

Name: Venlafaxine HCl
SKU: S1441
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S1441

Venlafaxine HCl(Wy 453 HCl) is an arylalkanolamine serotonin-norepinephrine reuptake inhibitor (SNRI), used to treat major depressive disorder (MDD), generalised anxiety disorder (GAD), panic disorder and social phobia.

Chemical Structure

Molecular Weight: 313.86

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel GluR MAO Beta Amyloid NMDAR P2 Receptor Trk receptor Notch Cannabinoid Receptor P-gp CaMK Opioid Receptor BACE Sigma Receptor FAAH Neurokinin Receptor OX Receptor CGRP Receptor BChE Adenosine Deaminase CCK receptor MT Receptor
Related Products	Dapoxetine Serotonin transporter Antibody [B14A13]

Chemical Information, Storage & Stability

Molecular Weight	313.86	Formula	C₁₇H₂₇NO₂·HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	99300-78-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Wy 453 HCl			Smiles	CN(C)CC(C1=CC=C(C=C1)OC)C2(CCCCC2)O.Cl

Solubility

In vitro
Batch:

DMSO : 63 mg/mL (200.72 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 63 mg/mL

Ethanol : 63 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.15mg/ml (10.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 63 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.45mg/ml (1.43mM)	Taking the 1 mL working solution as an example, add 50 μL of 9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	5-HT ^[1]
In vitro	Venlafaxine has a low potential to inhibit the metabolism of substrates for CYP2D6 such as imipramine and desipramine compared with several of the most widely used SSRIs, as well as the metabolism of substrates for several of the other major human hepatic P450s. ^[1] Venlafaxine inhibits binding to the human norepinephrine (NE) and serotonin (5-HT) transporters with K(i) values of 2480 nM and 82 nM, respectively, and with a K(i) ratio of 30. Venlafaxine has ED(50) values of 5.9 mg/kg and 94 mg/kg for blocking p-chloramphetamine- and 6-hydroxydopamine-induced monoamine depletion, respectively. ^[2]
In vivo	Venlafaxine induces a dose-dependent antinociceptive effect following i.p. administration with an ED50 of 46.7 mg/kg in mice. Venlafaxine-induced antinociception is significantly inhibited by naloxone, nor-BNI and naltrindole but not by beta-FNA or naloxonazine, implying involvement of kappa1- and delta-opioid mechanisms in mice. ^[3] Venlafaxine reverses hyperalgesia in rats with a fully developed neuropathic lesion. Venlafaxine also appears to have a mild non-specific analgesic effect that increased paw withdrawal latency (PWL) in the sham limb. ^[4]
References	[1] https://pubmed.ncbi.nlm.nih.gov/9205822/ [2] https://pubmed.ncbi.nlm.nih.gov/11750180/ [3] https://pubmed.ncbi.nlm.nih.gov/10505622/ [4] https://pubmed.ncbi.nlm.nih.gov/9252010/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06131268	Recruiting	Major Depressive Disorder\|Bipolar Affective Disorder Currently Depressed Moderate	Fondazione IRCCS Ca'' Granda Ospedale Maggiore Policlinico	March 1 2022	Phase 4
NCT04708834	Enrolling by invitation	Obsessive Compulsive Disorder	Biohaven Pharmaceuticals Inc.	March 30 2021	Phase 3
NCT03532477	Recruiting	Obesity Morbid	Norwegian University of Science and Technology\|St. Olavs Hospital\|Volvat Medisinsk Senter Stokkan\|Namsos Hospital\|Alesund Hospital	November 2 2016	--
NCT02637193	Completed	Healthy Subjects	Pfizer''s Upjohn has merged with Mylan to form Viatris Inc.\|Pfizer	December 2015	Phase 1
NCT02005107	Completed	Roux en Y Gastric Bypass\|Sleeve Gastrectomy	North Dakota State University\|Neuropsychiatric Research Institute Fargo North Dakota	December 2013	Phase 4
NCT01867255	Completed	Bariatric Surgery\|Gastric Bypass\|Roux-en-Y Gastric Bypass	Mayo Clinic	October 2013	Phase 1

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