| Field | Specification |
|---|---|
| Target | |
| Alternative names | CP 88059 hydrochloride monohydrate |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C21H24Cl2N4O2S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Ziprasidone hydrochloride monohydrate, also known as CP-88059 hydrochloride monohydrate, is an orally active, combined 5-HT and dopamine receptor antagonist[1]. It shows affinity for rat D2 (Ki = 4.8 nM), 5-HT2A (Ki = 0.42 nM) and 5-HT1A (Ki = 3.4 nM)[1]. It is supplied as a pink to red solid (C21H24Cl2N4O2S, MW 467.41) at 98.11% purity.
Physical & Chemical Properties
| CAS Number | 138982-67-9 |
|---|---|
| Molecular Formula | C21H24Cl2N4O2S |
| Molecular Weight | 467.41 g/mol |
| Purity | 98.11% |
| Appearance | Solid |
| Color | Pink to red |
| SMILES | O=C1CC2=CC(CCN3CCN(C4=NSC5=C4C=CC=C5)CC3)=C(Cl)C=C2N1.[H]Cl.O |
| Target | Rat 5-HT 2A, 5-HT 1A Receptor, 5-HT 2A Receptor, Rat 5-HT 1A Receptor, Rat D 2 Receptor |
| Signaling Pathway | GPCR/G Protein; Neuronal Signaling |
| Solubility | In Vitro: DMSO: 25 mg/mL (53.49 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | 4°C, sealed storage, away from moisture and light. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
Activity & Target
[1][2]
|
Rat 5-HT2A 0.42 nM (Ki) |
5-HT1A Receptor |
5-HT2A Receptor |
Rat 5-HT1A Receptor 3.4 nM (Ki) |
Rat D2 Receptor 4.8 nM (Ki) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 25 mg/mL (53.49 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture and light; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (5.35 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 2.5 mg/mL (5.35 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 2.5 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Data provided by the manufacturer.
In Vitro
Wild-type hERG current is blocked by Ziprasidone hydrochloride monohydrate (0-500 nM, 150 seconds)[2].
Cell Viability Assay[2]
| 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). |
In Vivo
Treatment with Ziprasidone hydrochloride monohydrate (oral gavage; 20 mg/kg; once daily; 7 weeks) leads to weight loss and low-level physical activity, as well as high resting energy expenditure and a greater thermogenic capacity on exposure to cold[3].
| Animal Model | Eight-week-old female Sprague-Dawley rats weighing 200 to 250 g[3] |
|---|---|
| Dosage | 20 mg/kg |
| Administration | Oral gavage; 20 mg/kg; once daily; 7 weeks |
| Result | Gained significantly less weight (P = 0.031), had a lower level of physical activity (P = 0.016), showed a higher resting energy expenditure (P < 0.001), and displayed a greater capacity for thermogenesis when subjected to cold (P < 0.001). |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. ACS Environ Au 2025 Aug 5;5(6):573-582. PMID: 41277996
Heterogeneity and concentration-dependence of ionic channel mechanisms underlying ventricular repolarization prolongation induced by atypical antipsychotics. Toxicol Appl Pharmacol 2026 Oct:515:117973. PMID: 42520893
Supramolecular Solvent Extraction for Doping Control Analysis of Prohibited Substances in Horse Urine. Drug Test Anal 2026 May;18(5):652-668. PMID: 41814125
A drug repurposing screen reveals dopamine signaling as a candidate therapeutic pathway for PIGA-CDG. bioRxiv 2026 Apr 18:2026.04.17.719256. PMID: 42039650
Research Square Preprint. 2021 Jul.
