Sertindole

Alias: Sertindolum; Serdolect; SerLect; Serdolect; Serlect; sertindole; Lu 23-174; Sertindole; Sertindol; Lu-23-174; sertindole hydrochloride

Cat No.:V6700 Purity: ≥98%

COA Product Data Instructions for use SDS

Sertindole (Sertindolum; Lu 23-174) is a potent antipsychotic medication and a neuroleptic drug.

Sertindole Chemical Structure CAS No.: 106516-24-9
Product category: 5-HT Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of Sertindole:

Sertindole-d4 (sertindole d4)

Official Supplier of:

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Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Sertindole (Sertindolum; Lu 23-174) is a potent antipsychotic medication and a neuroleptic drug. Sertindole exerts a potent antagonism at serotonin 5-HT2A, 5-HT2C, dopamine D2, and αl adrenergic receptors. Sertindole strongly binds to the αl adrenergic, dopamine D2, serotonin 5-HT2A, and 5-HT2C receptors. With a favorable metabolic profile, good EPS profile, and efficacy comparable to risperidone, sertindole presents a viable alternative for treating patients who are not responding to other treatment options. For patients who are intolerant to other antipsychotic medications, sertindole is an option as a second-line treatment due to concerns about cardiovascular safety. Sertindole is anticipated to be a highly beneficial supplement to the current therapeutic options for the management of psychotic disorders. Sertindole improves negative symptoms, and is also effective for the treatment of neuroleptic-resistant schizophrenia. Sertindole has a low incidence of extrapyramidal symptoms (EPS) and is generally well tolerated. Consequently, sertindole is a helpful option for treating schizophrenia in patients.

Biological Activity I Assay Protocols (From Reference)

Targets	5-HT_2A Receptor; 5-HT_2C Receptor
ln Vitro	Sertindole (0-100 μM; 48 h) reduces the growth of breast cancer cells[2]. Sertindole (0.8-27.6 μM; 48 h) inhibits the proliferation of numerous cancers in vitro[2]. Sertindole (5 μΜ and 10 μΜ; 24 h) inhibits breast cancer cell migration[2].
ln Vivo	Sertindole (10 mg/kg; once daily; 12 d) exhibits anti-tumor activity in vivo[2].
Cell Assay	Cell Line: SUM159 and MCF-10A cells Concentration: 0-100 μM Incubation Time: 48 hours Result: Showed IC50s of 9.2 µM and 27.6 µM for SUM159 and MCF-10A cells, respectively.
Animal Protocol	Immune-deficient Balb/c mice implanted MDA-MB-231 human TNBC cells 10 mg/kg Oral gavage; 10 mg/kg; once daily; 12 days
References	[1]. Sertindole : a review of its use in schizophrenia. CNS Drugs. 2006;20(3):233-55. [2]. Antiproliferative activities of the second-generation antipsychotic drug sertindole against breast cancers with a potential application for treatment of breast-to-brain metastases. Sci Rep. 2018 Oct 25;8(1):15753. [3]. Sertindole in the management of schizophrenia. J Cent Nerv Syst Dis. 2011 May 17;3:75-85.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C24H26CLFN4O
Molecular Weight	440.94
Exact Mass	440.18
Elemental Analysis	C, 65.37; H, 5.94; Cl, 8.04; F, 4.31; N, 12.71; O, 3.63
CAS #	106516-24-9
Related CAS #	Sertindole-d4; 1794737-42-0
Appearance	Solid powder
SMILES	C1CN(CCC1C2=CN(C3=C2C=C(C=C3)Cl)C4=CC=C(C=C4)F)CCN5CCNC5=O
InChi Key	GZKLJWGUPQBVJQ-UHFFFAOYSA-N
InChi Code	InChI=1S/C24H26ClFN4O/c25-18-1-6-23-21(15-18)22(16-30(23)20-4-2-19(26)3-5-20)17-7-10-28(11-8-17)13-14-29-12-9-27-24(29)31/h1-6,15-17H,7-14H2,(H,27,31)
Chemical Name	1-[2-[4-[5-chloro-1-(4-fluorophenyl)indol-3-yl]piperidin-1-yl]ethyl]imidazolidin-2-one
Synonyms	Sertindolum; Serdolect; SerLect; Serdolect; Serlect; sertindole; Lu 23-174; Sertindole; Sertindol; Lu-23-174; sertindole hydrochloride
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: ~25 mg/mL (~56.7 mM)
Solubility (In Vivo)	Solubility in Formulation 1: ≥ 2.5 mg/mL (5.67 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 (5.67 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. View More Solubility in Formulation 3: ≥ 2.5 mg/mL (5.67 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. (Please use freshly prepared in vivo formulations for optimal results.)

Solubility (In Vitro)

DMSO: ~25 mg/mL (~56.7 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.67 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 (5.67 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.

View More

Solubility in Formulation 3: ≥ 2.5 mg/mL (5.67 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.

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.2679 mL	11.3394 mL	22.6788 mL
	5 mM	0.4536 mL	2.2679 mL	4.5358 mL
	10 mM	0.2268 mL	1.1339 mL	2.2679 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

Mass

Concentration

Volume

Molecular Weight*

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

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
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?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

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
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

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Desired Reconstitution Concentration

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make 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 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.)

% DMSO

% Tween 80

% ddH₂O

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.

Note： (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
NCT00864045	Completed	Drug: Sertindole Drug: Olanzapine	Schizophrenia	H. Lundbeck A/S	March 2007	Phase 3
NCT00856583	Completed	Drug: Sertindole Drug: Risperidone	Schizophrenia	H. Lundbeck A/S	July 2002	Phase 3
NCT00345982	Completed	Drug: Serdolect Drug: placebo	Schizophrenia	University of Aarhus	September 2006	Not Applicable
NCT00763438	Completed	Drug: Sertindole	Schizophrenia	H. Lundbeck A/S	November 2007	Phase 4
NCT00654706	Completed	Drug: Sertindole Drug: Quetiapine	Schizophrenia Cognition	H. Lundbeck A/S	March 2008	Phase 3

Biological Data

Sertindole induces cell-lethal autophagy in SUM159 cells. Sci Rep . 2018 Oct 25;8(1):15753.
Sertindole induces apoptosis in SUM159 cells which is autophagy-associated. Sci Rep . 2018 Oct 25;8(1):15753.
Overexpression of 5-HT6 receptor suppresses sertindole-induced LC3 conversion and caspase-3 cleavage in SUM159 cells. Sci Rep . 2018 Oct 25;8(1):15753.
Inactivation of 5-HT6 receptor by its target-specific antagonist SB258585 augments LC3II conversion and caspase-3 cleavage in sertindole-treated SUM159 cells. Sci Rep . 2018 Oct 25;8(1):15753.