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> Ziprasidone [146939-27-7]

Ziprasidone [146939-27-7]

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Ziprasidone (CP-88059), an orally active antipsychotic agent, is a combined 5-HT and dopamine receptor antagonist. Ziprasidone mesylate trihydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM).

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Ziprasidone Chemical Structure

Ziprasidone Chemical Structure

CAS No. : 146939-27-7

This product is a controlled substance and not for sale in your territory.

Based on 1 publication(s) in Google Scholar

Other Forms of Ziprasidone:

  • Ziprasidone-d8 In-stock
  • Ziprasidone hydrochloride monohydrate In-stock
  • Ziprasidone hydrochloride Obtenir un devis
  • Ziprasidone mesylate trihydrate Obtenir un devis
  • Ziprasidone mesylate Obtenir un devis

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Description

Ziprasidone (CP-88059), an orally active antipsychotic agent, is a combined 5-HT and dopamine receptor antagonist[1]. Ziprasidone mesylate trihydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM)[1].

IC50 & Target[1][2]

Rat 5-HT1A Receptor

3.4 nM (Ki)

human 5-HT1A Receptor

2.5 nM (Ki)

Rat D2 Receptor

4.8 nM (Ki)

Rat 5-HT2A

0.42 nM (Ki)

In Vitro

Ziprasidone (0-500 nM, 150 seconds) blocks wild-type hERG current[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ziprasidone Related Antibodies

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

Ziprasidone (oral gavage; 20 mg/kg; once daily; 7 weeks) results in weight loss, low level physical activity, high resting energy expenditure and greater capacity for thermogenesis when subjected to cold[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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).
Essai clinique
Masse moléculaire

412.94

Formule

C21H21ClN4OS
CAS No.

146939-27-7
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC2=C(CC(N2)=O)C=C1CCN(CC3)CCN3C4=NSC5=C4C=CC=C5
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvant et solubilité
In Vitro: 

DMSO : 13.5 mg/mL (32.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Calculateur de molarité

  • Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.35 mg/mL (3.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.35 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.35 mg/mL (3.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.35 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
Références

  • [1]. Rollema H, et al. 5-HT(1A) receptor activation contributes to ziprasidone-induced dopamine release in the rat prefrontal cortex. Biol Psychiatry. 2000;48(3):229-237.  [Content Brief]

    [2]. Zhi Su, et al. Block of hERG channel by ziprasidone: biophysical properties and molecular determinants. Biochem Pharmacol. 2006 Jan 12;71(3):278-86.  [Content Brief]

    [3]. Subin Park, et al. The effect of ziprasidone on body weight and energy expenditure in female rats. Metabolism. 2012 Jun;61(6):787-93.  [Content Brief]

  • [1]. Rollema H, et al. 5-HT(1A) receptor activation contributes to ziprasidone-induced dopamine release in the rat prefrontal cortex. Biol Psychiatry. 2000;48(3):229-237.

    [2]. Zhi Su, et al. Block of hERG channel by ziprasidone: biophysical properties and molecular determinants. Biochem Pharmacol. 2006 Jan 12;71(3):278-86.

    [3]. Subin Park, et al. The effect of ziprasidone on body weight and energy expenditure in female rats. Metabolism. 2012 Jun;61(6):787-93.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4217 mL 12.1083 mL 24.2166 mL 60.5415 mL
5 mM 0.4843 mL 2.4217 mL 4.8433 mL 12.1083 mL
10 mM 0.2422 mL 1.2108 mL 2.4217 mL 6.0541 mL
15 mM 0.1614 mL 0.8072 mL 1.6144 mL 4.0361 mL
20 mM 0.1211 mL 0.6054 mL 1.2108 mL 3.0271 mL
25 mM 0.0969 mL 0.4843 mL 0.9687 mL 2.4217 mL
30 mM 0.0807 mL 0.4036 mL 0.8072 mL 2.0180 mL
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Ziprasidone Related Classifications

Help & FAQs

Keywords:

Ziprasidone146939-27-7CP-88059CP88059CP 880595-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine Receptorantipsychotic agent5-HT receptorserotonindopamine receptorHEK-293Inhibitorinhibitorinhibit

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