Name: Ziprasidone HCl
Brand: Selleck Chemicals
SKU: S1444
Availability: InStock
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Batch: S144401 DMSO]90 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.01%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS/MSDS
Datasheet

99.01

Related Targets	Adrenergic Receptor AChR COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other 5-HT Receptor Inhibitors	Serotonin Hydrochloride (5-HT HCl) WAY-100635 Maleate Puerarin SB269970 HCl Ketanserin BRL-15572 Dihydrochloride Nuciferine RS-127445 Flopropione Azacyclonol

Solubility

In vitro
Batch:

DMSO : 90 mg/mL (200.26 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : 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.
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.	0.325mg/ml (0.72mM)	Taking the 1 mL working solution as an example, add 50 μL of 6.5 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.

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

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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.

Chemical Information, Storage & Stability

Molecular Weight	449.4	Formula	C₂₁H₂₁ClN₄OS·HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	122883-93-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CP-88059			SMILES	C1CN(CCN1CCC2=C(C=C3C(=C2)CC(=O)N3)Cl)C4=NSC5=CC=CC=C54.Cl

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	5-HT receptor Dopamine receptor
In vitro	Ziprasidone has high affinity for human 5-HT receptors and for human dopamine D(2) receptors. Ziprasidone is a 5-HT(1A) receptor agonist and an antagonist at 5-HT(2A), 5-HT(2C) and 5-HT(1B/1D) receptors. Ziprasidone inhibits neuronal uptake of 5-HT and norepinephrine comparable to the antidepressant imipramine. Ziprasidone blocks wild-type hERG current in a voltage- and concentration-dependent manner with IC(50) of 120nM in stably transfected HEK-293 cells. Ziprasidone shows minimal tonic block of hERG current estimated during a depolarizing voltage (-20 or +30mV) or evaluated by the envelope of tails test (+30mV). Ziprasidone significantly increases the time constant of the slow component of hERG current deactivation (at -50mV).
In vivo	Ziprasidone exhibits less potent block of wild-type hERG current with IC(50) of 2.8 mM in Xenopus oocytes. Ziprasidone suppresses the significant increases in food intake produced by olanzapine, indicating that it has an intrinsic protective mechanism against drug-induced increases in food intake in rats. Ziprasidone results in a notable increase in NGF and ChAT immunoreactivity in the dentate gyrus (DG), CA1, and CA3 areas of the hippocampus of rats. Ziprasidone dose-dependently slows raphe unit activity (ED50 = 300 mg/kg i.v.) as does the atypical antipsychotics clozapine (ED50 = 250 mg/kg i.v.) and olanzapine (ED50 = 1000 mg/kg i.v.) in anesthetized rats.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11513838/ [2] https://pubmed.ncbi.nlm.nih.gov/16325148/ [3] https://pubmed.ncbi.nlm.nih.gov/15556160/ [4] https://pubmed.ncbi.nlm.nih.gov/16702442/ [5] https://pubmed.ncbi.nlm.nih.gov/10516958/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-07-08)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03781115	ACTIVE_NOT_RECRUITING	Schizophrenia	University of Arizona	2017-11-20	PHASE1
NCT04446234	UNKNOWN	Schizophrenia	Shanghai Mental Health Center	2021-05	PHASE4
NCT03837860	TERMINATED	Opioid Abuse, Unspecified; Opioid Dependence	The University of Texas Health Science Center at San Antonio	2019-04-01	EARLY_PHASE1
NCT03768726	TERMINATED	Bipolar Disorder	Pfizer's Upjohn has merged with Mylan to form Viatris Inc.	2018-12-21	PHASE3
NCT02075047	TERMINATED	Bipolar Disorder	Pfizer's Upjohn has merged with Mylan to form Viatris Inc.	2014-05-23	PHASE3
NCT03011645	TERMINATED	Cardiovascular Diseases	Duke University	2018-05-24	PHASE1

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Ziprasidone HCl 5-HT Receptor antagonist

Chemical Structure

Molecular Weight: 449.4