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100mg |
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250mg |
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500mg |
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1g |
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2g |
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Ziprasidone (CP-88,059; CP 88059; CP-88,059-01; Geodon; Zeldox; Zipwell) is a dopamine and serotonin (5-HT) receptor antagonist with antipsychotic effects. It is authorized for the treatment of acute mania, mixed states linked to bipolar disorder, and schizophrenia and bipolar illness. When treating schizophrenia patients who respond best to treatment consisting solely of ziprasidone, its intramuscular injection form is authorized for use in cases of acute agitation. According to theories about ziprasidone's mode of action, serotonin type 2 (5HT2) and dopamine type 2 (D2) antagonistic interactions together mediate the drug's effectiveness in treating schizophrenia. The exact mechanism by which ziprasidone treats bipolar disorder is unknown, as it is with other medications that are effective in treating the condition.
Targets |
Rat 5-HT1A Receptor ( Ki = 3.4 nM ); human 5-HT1A Receptor ( Ki = 2.5 nM ); Rat D2 Receptor ( Ki = 4.8 nM ); Rat 5-HT2A ( Ki = 0.42 nM )
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ln Vitro |
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ln Vivo |
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Cell Assay |
Cell Line: HEK-293 cells
Concentration: 0-500 nM Incubation Time: 150 seconds Result: Blocked wild-type hERG current in a voltage- and concentration-dependent manner (IC50 = 120 nm). |
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Animal Protocol |
Eight-week-old female Sprague-Dawley rats weighing 200 to 250 g
20 mg/kg Oral gavage; 20 mg/kg; once daily; 7 weeks |
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References |
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Molecular Formula |
C21H21CLN4OS
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Molecular Weight |
412.94
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Exact Mass |
412.11
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Elemental Analysis |
C, 61.08; H, 5.13; Cl, 8.58; N, 13.57; O, 3.87; S, 7.76
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CAS # |
146939-27-7
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Related CAS # |
Ziprasidone-d8; 1126745-58-1; Ziprasidone hydrochloride monohydrate; 138982-67-9; Ziprasidone hydrochloride; 122883-93-6; Ziprasidone mesylate trihydrate; 199191-69-0; Ziprasidone mesylate; 185021-64-1
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Appearance |
Solid powder
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SMILES |
C1CN(CCN1CCC2=C(C=C3C(=C2)CC(=O)N3)Cl)C4=NSC5=CC=CC=C54
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InChi Key |
MVWVFYHBGMAFLY-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C21H21ClN4OS/c22-17-13-18-15(12-20(27)23-18)11-14(17)5-6-25-7-9-26(10-8-25)21-16-3-1-2-4-19(16)28-24-21/h1-4,11,13H,5-10,12H2,(H,23,27)
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Chemical Name |
5-[2-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]ethyl]-6-chloro-1,3-dihydroindol-2-one
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Synonyms |
CP 88059; CP88059; CP-88,059-01; CP88059 hydrochloride; CP-88059; CP-88,059; Ziprasidone HCl; Geodon; Zeldox; Zipwell
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HS Tariff Code |
2934.99.9001
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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)
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Solubility (In Vitro) |
DMSO: ~13.5 mg/mL (~32.7 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.35 mg/mL (3.27 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 13.5 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: ≥ 1.35 mg/mL (3.27 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 13.5 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: ≥ 1.35 mg/mL (3.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4217 mL | 12.1083 mL | 24.2166 mL | |
5 mM | 0.4843 mL | 2.4217 mL | 4.8433 mL | |
10 mM | 0.2422 mL | 1.2108 mL | 2.4217 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.
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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03781115 | Recruiting | Drug: Ziprasidone Drug: Olanzapine |
Schizophrenia | University of Arizona | November 20, 2017 | Phase 1 |
NCT01714011 | Completed | Drug: Ziprasidone Drug: Aripiprazole |
Schizophrenia | University of Malaya | May 2009 | Phase 4 |
NCT01581866 | Completed | Drug: Ziprasidone Hydrochloride | Healthy | Dr. Reddy's Laboratories Limited | November 2004 | Phase 1 |
NCT01581879 | Completed | Drug: Ziprasidone Hydrochloride | Healthy | Dr. Reddy's Laboratories Limited | November 2004 | Phase 1 |
NCT01198353 | Completed | Drug: Ziprasidone | Schizoaffective Disorder Schizophrenia |
Soonchunhyang University Hospital | September 2010 | Phase 4 |