Ziprasidone HCl (CP-88059)

Alias: CP-88059; CP88059; CP88059 mesylate; Ziprasidone mesylate; CP 88059; CP-88,059; CP-88,059-01; Geodon; Zeldox; Zipwell
Cat No.:V0983 Purity: ≥98%
Ziprasidone (CP 88059; CP-88,059; CP-88,059-01; Geodon; Zeldox; Zipwell) HCl, the hydrochloride salt of Ziprasidone, is a novel and potent dopamine and serotonin (5-HT) receptor antagonist with antipsychotic effects.
Ziprasidone HCl (CP-88059) Chemical Structure CAS No.: 122883-93-6
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 Ziprasidone HCl (CP-88059):

  • Ziprasidone free base
  • Ziprasidone D8
  • Ziprasidone HCl hydrate
  • Ziprasidone mesylate trihydrate
  • Ziprasidone mesylate
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Ziprasidone (CP 88059; CP-88,059; CP-88,059-01; Geodon; Zeldox; Zipwell) HCl, the hydrochloride salt of Ziprasidone, is a novel and potent 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.

Biological Activity I Assay Protocols (From Reference)
Targets
Rat 5-HT2A ( Ki = 0.42 nM ); Rat 5-HT1A Receptor ( Ki = 3.4 nM ); Rat D2 Receptor ( Ki = 4.8 nM )
ln Vitro

In vitro activity: Ziprasidone has high affinity for human 5-HT receptors and for human dopamine D(2) receptors. Ziprasidone exhibits agonistic properties towards 5-HT(1A) receptors and antagonistic properties towards 5-HT(2A), 5-HT(2C), and 5-HT(1B/1D) receptors. Similar to the antidepressant imipramine, ziprasidone inhibits the uptake of 5-HT and norepinephrine by neurons. [1] In stable transfected HEK-293 cells, ziprasidone inhibits wild-type hERG current in a concentration- and voltage-dependent manner with an IC(50) of 120 nM. When assessed using the envelope of tails test (+30mV) or during a depolarizing voltage (-20 or +30mV), ziprasidone exhibits a minimal tonic block of hERG current. At -50mV, ziprasidone considerably lengthens the slow component of hERG current deactivation's time constant. [2]

ln Vivo
Ziprasidone blocks wild-type hERG current less potently, with an IC(50) of 2.8 mM in Xenopus oocytes. [2] Ziprasidone has an inherent protective mechanism against drug-induced increases in food intake in rats, as evidenced by its ability to suppress the significant increases in food intake caused by olanzapine[2]. Rat hippocampal regions (CA1, CA3, and dentate gyrus, DG) exhibit significant increases in NGF and ChAT immunoreactivity when treated with ziprasidone [3]. As with the atypical antipsychotics clozapine (ED50 = 250 mg/kg i.v.) and olanzapine (ED50 = 1000 mg/kg i.v.), ziprasidone dose-dependently slows raphe unit activity in anesthetized rats.[5]
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).
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
References

[1]. Eur J Pharmacol . 2001 Aug 17;425(3):197-201.

[2]. Biochem Pharmacol . 2006 Jan 12;71(3):278-86.

[3]. Eur J Pharmacol . 2004 Nov 28;505(1-3):253-4.

[4]. J Pharmacol Exp Ther . 2006 Aug;318(2):709-24.

[5]. Neuropsychopharmacology . 1999 Nov;21(5):622-31.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H22CL2N4OS
Molecular Weight
449.4
Exact Mass
448.09
Elemental Analysis
C, 56.13; H, 4.93; Cl, 15.78; N, 12.47; O, 3.56; S, 7.13
CAS #
122883-93-6
Appearance
Solid powder
SMILES
C1CN(CCN1CCC2=C(C=C3C(=C2)CC(=O)N3)Cl)C4=NSC5=CC=CC=C54.Cl
InChi Key
NZDBKBRIBJLNNT-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H21ClN4OS.ClH/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);1H
Chemical Name
5-[2-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]ethyl]-6-chloro-1,3-dihydroindol-2-one;hydrochloride
Synonyms
CP-88059; CP88059; CP88059 mesylate; Ziprasidone mesylate; CP 88059; CP-88,059; CP-88,059-01; Geodon; Zeldox; Zipwell
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: ~90 mg/mL (~200.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2252 mL 11.1259 mL 22.2519 mL
5 mM 0.4450 mL 2.2252 mL 4.4504 mL
10 mM 0.2225 mL 1.1126 mL 2.2252 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.

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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.

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Clinical Trial Information
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
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