Sertraline HCl

Alias: CP-51974-1 HCl; CP51974-1 HCl; Sertraline Hydrochloride; Sertraline HCl; Sealdin; Adjuvin; Atruline; CP 51,974-1; Cp-51,974-1; CP 51974-1 HCl; CP 51,974; CP51,974; CP-51,974; Gladem; Tatig; Tresleen; Zoloft
Cat No.:V1029 Purity: ≥98%
Sertraline HCl (formerly CP 51,974-1; CP 51974-1; CP-51,974; trade names: Sealdin; Adjuvin; Atruline; Gladem; Tatig; Tresleen; Zoloft), the hydrochloride salt of Sertraline, is a potent and marketed antidepressant drug acting as a 5-HT serotonin receptor antagonist with Ki of 13 nM.
Sertraline HCl Chemical Structure CAS No.: 79559-97-0
Product category: 5-HT Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
250mg
500mg
1g
2g
5g
10g
Other Sizes

Other Forms of Sertraline HCl:

  • (±)-cis-Sertraline-d3 hydrochloride ((±)-Sertraline d3 hydrochloride (hydrochloride))
  • rel-Sertraline-d3 hydrochloride (sertraline d3 hydrochloride (hydrochloride))
  • Sertraline (CP-51974-1)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Sertraline HCl (formerly CP 51,974-1; CP 51974-1; CP-51,974; trade names: Sealdin; Adjuvin; Atruline; Gladem; Tatig; Tresleen; Zoloft), the hydrochloride salt of Sertraline, is a potent and marketed antidepressant drug acting as a 5-HT serotonin receptor antagonist with Ki of 13 nM. Sertraline binds to the serotonin transporter with an affinity of Ki=2.8 nM, making it primarily a serotonin reuptake inhibitor (SRI). Compared to NE uptake, sertraline is more selective than fluvoxamine, zimelidine, norzimelidine, fluoxetine, or chlorimipramine in inhibiting 5-HT uptake. Sertraline, in contrast to these agents, is less selective in preventing 5-HT uptake than DA uptake. Moreover, sertraline (<50 nmol/L) inhibits the reuptake of dopamine. Its action is only 10% of its potency as a monoamine reuptake inhibitor, and this is not thought to be a tight binding. Its SRI potency ranges from 1% to 10% for α1-adrenoreceptor antagonists and 5% for σ1 receptor agonists.

Biological Activity I Assay Protocols (From Reference)
Targets
5-HT ( Ki = 13 nM )
ln Vitro

In vitro activity: Sertraline demonstrates superior selectivity in blocking 5-HT uptake in comparison to NE uptake when compared to fluvoxamine, zimelidine, norzimelidine, fluoxetine, or chlorimipramine. Nevertheless, in comparison to these agents, sertraline is less selective in preventing 5-HT uptake than DA uptake.[1]

ln Vivo
Sertraline HCl (32μmol/kg i.p.) reduces serotonin uptake by more than 50% in rat striatal synaptosomes. When it comes to reversing the 5-HT depletion induced by PCA, sertraline HCl is 60 times more potent than amitriptyline and 6 times more potent than chlorimipramine. Whole blood's serotonin content dropped after receiving repeated acute doses of sertraline. When antidepressant mice are used in the Porsolt swim test, sertraline HCl significantly decreases their immobility. Sertraline HCl reduces the binding of [3H]dihydroalprenolol to cortical membranes and the cyclic AMP response of limbic forebrain adenylate cyclase to norepinephrine in rats after repeated dosing.[1]
Animal Protocol
Aromatase-knockout (Ar−/−) mice
10 mg/kg
A single i.p. administration
References

[1]. J Pharmacol Exp Ther . 1983 Sep;226(3):686-700.

[2]. J Pharmacol Exp Ther . 1976 Dec;199(3):649-61.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H18CL3N
Molecular Weight
342.69
Exact Mass
341.05
Elemental Analysis
C, 59.58; H, 5.29; Cl, 31.04; N, 4.09
CAS #
79559-97-0
Related CAS #
(±)-cis-Sertraline-d3 hydrochloride; 1217741-83-7; rel-Sertraline-d3 hydrochloride; 1330180-66-9; 79617-96-2
Appearance
White to off-white solid powder
SMILES
CN[C@H]1CC[C@H](C2=CC=CC=C12)C3=CC(=C(C=C3)Cl)Cl.Cl
InChi Key
BLFQGGGGFNSJKA-XHXSRVRCSA-N
InChi Code
InChI=1S/C17H17Cl2N.ClH/c1-20-17-9-7-12(13-4-2-3-5-14(13)17)11-6-8-15(18)16(19)10-11;/h2-6,8,10,12,17,20H,7,9H2,1H3;1H/t12-,17-;/m0./s1
Chemical Name
(1S,4S)-4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalen-1-amine;hydrochloride
Synonyms
CP-51974-1 HCl; CP51974-1 HCl; Sertraline Hydrochloride; Sertraline HCl; Sealdin; Adjuvin; Atruline; CP 51,974-1; Cp-51,974-1; CP 51974-1 HCl; CP 51,974; CP51,974; CP-51,974; Gladem; Tatig; Tresleen; Zoloft
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 50~69 mg/mL (145.9~201.3 mM)
Water: <1 mg/mL
Ethanol: ~15 mg/mL (~43.8 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (7.30 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (7.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 30% PEG400+0.5% Tween80+5% Propylene glycol : 5 mg/mL

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.9181 mL 14.5904 mL 29.1809 mL
5 mM 0.5836 mL 2.9181 mL 5.8362 mL
10 mM 0.2918 mL 1.4590 mL 2.9181 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00667121 Active
Recruiting
Drug: sertraline hydrochloride
Drug: venlafaxine
Drug: gabapentin
Breast Cancer
Depression
Hot Flashes
Mayo Clinic March 16, 2011 N/A
NCT05930912 Active
Recruiting
Drug: sertraline 50mg
Drug: Duloxetine 20 MG
PTSD
OCD
Grief
Yang I. Pachankis, PhD June 1, 2023 N/A
NCT04963257 Recruiting Drug: sertraline fluvoxamine
Drug: sertraline
OCD Second Affiliated Hospital,
School of Medicine,
Zhejiang University
January 1, 2020 Phase 4
NCT04221997 Recruiting Drug: sertraline Anxiety Disorders University of Cincinnati November 1, 2019 Phase 4
NCT05646693 Recruiting Drug: Sertraline
Drug: Placebo
SSRI
Oxidative Stress
Psychiatric Drugs
University of Guadalajara December 1, 2022 Phase 2
Biological Data
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