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Sertraline HCl Serotonin Transporter inhibitor

Name: Sertraline HCl
Brand: Selleck Chemicals
SKU: S4053
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S4053

Sertraline HCl (CP-51974-1) is a 5-HT antagonist with K_i of 13 nM.

Chemical Structure

Molecular Weight: 342.69

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

Quality Control

Batch: Purity: 99.97%

99.97

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

Chemical Information, Storage & Stability

Molecular Weight	342.69	Formula	C₁₇H₁₇Cl₂N.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	79559-97-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CP-51974-1 HCl			Smiles	CNC1CCC(C2=CC=CC=C12)C3=CC(=C(C=C3)Cl)Cl.Cl

Solubility

In vitro
Batch:

DMSO : 69 mg/mL (201.34 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.
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.
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	30%PEG400 1 0.5%Tween80 2 5%propylene glycol Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (14.59mM)	Taking the 1 mL working solution as an example, add 300 μL of 16.67 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O Dilute to 1 mL. 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] 13 nM(Ki)
In vitro	Sertraline HCl exhibits better selectivity for inhibiting 5-HT uptake relative to NE uptake than fluvoxamine, zimelidine, norzimelidine, fluoxetine or chlorimipramine. However, this compound is less selective for blocking 5-HT uptake, relative to DA uptake than these agents. ^[1]
In vivo	Sertraline HCl (32μmol/kg i.p.) inhibits serotonin uptake into striatal synaptosomes from rats by more than 50%. This compound is 6 times more potent than chlorimipramine and 60 times more potent than amitriptyline in reversing the 5-HT depletion elicited by PCA. Acute and repeated dosing of sertraline decreased serotonin content of whole blood. This chemical strongly reduces immobility of mice in the Porsolt swim test for antidepressants. After repeated dosing in rats, it diminishes the cyclic AMP response of limbic forebrain adenylate cyclase to norepinephnne, as well as the binding of [³H]dihydroalprenolol to cortical membranes. ^[1]
References	[1] http://www.ncbi.nlm.nih.gov/pubmed/?term=6310078 [2] http://www.ncbi.nlm.nih.gov/pubmed/?term=994022

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05730062	Not yet recruiting	Opioid Induced Respiratory Depression\|Depressive Disorder\|Anxiety Disorders	Leiden University Medical Center	March 15 2023	Phase 1
NCT05189977	Terminated	Post-traumatic Stress Disorder (PTSD)	Otsuka Pharmaceutical Development & Commercialization Inc.\|Iqvia Pty Ltd	September 7 2022	Phase 1
NCT05210153	Recruiting	Depressive Disorder Major	University of Belgrade\|Clinical Centre of Serbia\|Institute of Mental Health Serbia\|Military Medical Academy Belgrade Serbia	July 16 2020	--
NCT04147000	Terminated	Overweight\|Depression\|Anxiety Disorders	Linkoeping University\|Örebro University Sweden	January 1 2020	--
NCT03711708	Completed	Healthy	Pfizer''s Upjohn has merged with Mylan to form Viatris Inc.\|Pfizer	November 6 2018	Phase 4

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