Ziprasidone HCl

製品コードS1444 バッチS144401

印刷

化学情報

Chemical Structure Synonyms CP-88059 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H21ClN4OS·HCl
分子量 449.4 CAS No. 122883-93-6
Solubility (25°C)* 体外 DMSO 90 mg/mL (200.26 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.325mg/ml (0.72mM) Taking the 1 mL working solution as an example, add 50 μL of 6.5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Ziprasidone HCl（CP-88059）は、新規で強力なdopamine およびserotonin (5-HT) receptor アンタゴニストであり、統合失調症や双極性障害の治療に用いられます。
in vitro Ziprasidone has high affinity for human 5-HT receptors and for human dopamine D(2) receptors. Ziprasidone is a 5-HT(1A) receptor agonist and an antagonist at 5-HT(2A), 5-HT(2C) and 5-HT(1B/1D) receptors. Ziprasidone inhibits neuronal uptake of 5-HT and norepinephrine comparable to the antidepressant imipramine. Ziprasidone blocks wild-type hERG current in a voltage- and concentration-dependent manner with IC(50) of 120nM in stably transfected HEK-293 cells. Ziprasidone shows minimal tonic block of hERG current estimated during a depolarizing voltage (-20 or +30mV) or evaluated by the envelope of tails test (+30mV). Ziprasidone significantly increases the time constant of the slow component of hERG current deactivation (at -50mV).
in vivo Ziprasidone exhibits less potent block of wild-type hERG current with IC(50) of 2.8 mM in Xenopus oocytes. Ziprasidone suppresses the significant increases in food intake produced by olanzapine, indicating that it has an intrinsic protective mechanism against drug-induced increases in food intake in rats. Ziprasidone results in a notable increase in NGF and ChAT immunoreactivity in the dentate gyrus (DG), CA1, and CA3 areas of the hippocampus of rats. Ziprasidone dose-dependently slows raphe unit activity (ED50 = 300 mg/kg i.v.) as does the atypical antipsychotics clozapine (ED50 = 250 mg/kg i.v.) and olanzapine (ED50 = 1000 mg/kg i.v.) in anesthetized rats.

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/11513838/
  • https://pubmed.ncbi.nlm.nih.gov/16325148/
  • https://pubmed.ncbi.nlm.nih.gov/15556160/
  • https://pubmed.ncbi.nlm.nih.gov/16702442/
  • https://pubmed.ncbi.nlm.nih.gov/10516958/

カスタマーフィードバック

Data from [Data independently produced by , , Nature, 2018, 560(7718):372-376]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Antiviral activity evaluation of pharmaceutical drugs, newly synthesized compounds and fragments against SARS-CoV-2 in vitro [ UNIVERSITY OF PÉCS, 2023, ] PubMed: None
A Low Dose of Aripiprazole Has the Strongest Sensitization Effect Among 19 Repositioned Bipolar Drugs in P-gp-overexpressing Drug-resistant Cancer Cells [ Anticancer Res, 2021, 41(2):687-697] PubMed: 33517273
Atypical Antipsychotic Drug Ziprasidone Protects against Rotenone-Induced Neurotoxicity: An In Vitro Study [ Molecules, 2020, 25(18)E4206] PubMed: 32937854
Accumulation of 8,9-unsaturated sterols drives oligodendrocyte formation and remyelination [Hubler Z, et al. Nature, 2018, 560(7718):372-376] PubMed: 30046109
Antiproliferative activities of the second-generation antipsychotic drug sertindole against breast cancers with a potential application for treatment of breast-to-brain metastases. [ Sci Rep, 2018, 8(1):15753] PubMed: 30361678
In Vitro Micropatterned Human Pluripotent Stem Cell Test (µP-hPST) for Morphometric-Based Teratogen Screening. [Xing J, et al. Sci Rep, 2017, 7(1):8491] PubMed: 28819231

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。