For research use only.
Licensed by Pfizer Catalog No.S1444 Synonyms: CP-88059
Molecular Weight(MW): 449.4
Ziprasidone HCl is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder.
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|Description||Ziprasidone HCl is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder.|
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. |
-  Schmidt AW, et al. Eur J Pharmacol, 2001, 425(3), 197-201.
-  Su Z, et al. Biochem Pharmacol, 2006, 71(3), 278-286.
-  Kirk SL, et al. Eur J Pharmacol, 2004, 505(1-3), 253-254.
|In vitro||DMSO||90 mg/mL (200.26 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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||ul||Number of animals|
|Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (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.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01245348||Completed||Genetic: SULT4A1-1 genetic test||Schizophrenia|Bipolar Disorder||Medco Health Solutions Inc.|SureGene LLC||December 2010||--|
|NCT01714011||Completed||Drug: Ziprasidone|Drug: Aripiprazole||Schizophrenia||University of Malaya||May 2009||Phase 4|
|NCT00835107||Completed||Drug: ziprasidone hydrochloride|Drug: placebo||Depression Bipolar||Queen''s University|Providence Health & Services|Pfizer|MDS Pharma Services||February 2009||Phase 4|
|NCT00676429||Completed||Drug: Ziprasidone Hydrochloride|Drug: Placebo||Conduct Disorder|Oppositional Defiant Disorder||University Hospital Freiburg|Pfizer||July 2006||Phase 2|
|NCT00148564||Completed||Drug: olanzapine|Drug: Ziprasidone||Schizophrenia||Charite University Berlin Germany||March 2004||Phase 4|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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