ジプラシドン
Based on 5 publication(s) in Google Scholar
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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.31%
- CAS 番号: 146939-27-7
- 分子式: C21H21ClN4OS
- 分子量:412.94
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
|
5-HT1A Receptor |
5-HT2A Receptor |
Rat 5-HT1A Receptor 3.4 nM (Ki) |
Rat D2 Receptor 4.8 nM (Ki) |
Rat 5-HT2A 0.42 nM (Ki) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| WI-38 | CC50 |
>100 μM
Compound: Ziprasidone
|
Cytotoxicity against human WI38 cells assessed as reduction in cellular DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay
Cytotoxicity against human WI38 cells assessed as reduction in cellular DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay
|
[PMID: 17893158] |
| WI-38 | EC50 |
>100 μM
Compound: Ziprasidone
|
Antiviral activity against BKV Gardner ATCC VR837 infected in human WI38 cells assessed as reduction in viral DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay
Antiviral activity against BKV Gardner ATCC VR837 infected in human WI38 cells assessed as reduction in viral DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay
|
[PMID: 17893158] |
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.
-
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).
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).
化学情報
-
CAS 番号 146939-27-7
-
性状 Solid
-
分子量 412.94
-
分子式 C21H21ClN4OS
-
Color White to off-white
-
SMILES
ClC1=CC2=C(CC(N2)=O)C=C1CCN(CC3)CCN3C4=NSC5=C4C=CC=C5
-
別名
Ziprasidone; CP-88059
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
-
Journal Impact Factor
-
Most Recent
-
ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
-
Drug Test Anal
Supramolecular Solvent Extraction for Doping Control Analysis of Prohibited Substances in Horse Urine. [Abstract]2026 May;18(5):652-668. PMID: 41814125 -
bioRxiv
A drug repurposing screen reveals dopamine signaling as a candidate therapeutic pathway for PIGA-CDG. [Abstract]2026 Apr 18:2026.04.17.719256. PMID: 42039650 -
溶剤 & 溶解度
DMSO : 13.33 mg/mL (32.28 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
純度とドキュメンテーション
-
データシート (276 KB)
-
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
-
取扱説明書 (2659 KB)
参考文献
[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]
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 |
Ziprasidone 関連分類
HY-14542 関連分類
Powered by Bioz