Clozapine

製品コードS2459 バッチS245904

印刷

化学情報

Chemical Structure Synonyms HF 1854, LX 100-129 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C18H19ClN4
分子量 326.82 CAS No. 5786-21-0
Solubility (25°C)* 体外 DMSO 65 mg/mL (198.88 mM)
Ethanol 22 mg/mL (67.31 mM)
Water 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 Corn oil

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。

 5.000mg/ml (15.30mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
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。

 3.750mg/ml (11.47mM) Taking the 1 mL working solution as an example, add 50 μL of 75 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 Clozapine (HF 1854, LX 100-129) is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.
in vitro Clozapine (10, 20 mg/kg) significantly increases the number of Fos-positive neurons in the nucleus accumbens, medial prefrontal cortex and lateral septal nucleus. [1] This compound induces zif268 but not c-fos mRNA in rat striatum, while Haloperidol induces c-Fos-like immunoreactivity in the caudate-putamen. [2] It is more selective for D4 receptors compared to D2 receptors. This chemical is a mixed but weak D1/D2 antagonist. [3] It produces a marked facilitation (300-400%) of NMDA-evoked responses in a concentration-dependent manner with EC50 of 14 nM. This compound, but not haloperidol, produces bursts of excitatory postsynaptic potentials (EPSPs), which are blocked by glutamate receptor antagonists, suggesting that these EPSPs are the result of increasing release of excitatory amino acids. [4] It is a full agonist at the muscarinic M4 receptor (EC50 = 11 nM), producing inhibition of forskolin-stimulated cAMP accumulation. This chemical potently antagonizes agonist-induced responses at the other four muscarinic receptor subtypes. [5]
in vivo Clozapine exhibits an "inverted-U" shaped dose-response curve, reversing the apomorphine-induced loss of prepulse inhibition (PPI) at low doses but not at high doses in the rats. This compound decreases PPI independent of apomorphine treatment in the rats. [6]

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/1347406/
  • https://pubmed.ncbi.nlm.nih.gov/1374894/
  • https://pubmed.ncbi.nlm.nih.gov/8602893/
  • https://pubmed.ncbi.nlm.nih.gov/9336328/
  • https://pubmed.ncbi.nlm.nih.gov/7895765/
  • https://pubmed.ncbi.nlm.nih.gov/1825226/

カスタマーフィードバック

, , Drug Metab Dispos, 2015, 43(7):1147-53.

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：

Repurposing neuroleptics: clozapine as a novel, adjuvant therapy for melanoma brain metastases [ Clin Exp Metastasis, 2025, 42(2):12] PubMed: 39856383
Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805] PubMed: 39581704
Amisulpride as a potential disease-modifying drug in the treatment of tauopathies [ Alzheimers Dement, 2023, 10.1002/alz.13090] PubMed: 37218673
Clozapine suppresses NADPH oxidase activation, counteracts cytosolic H2O2, and triggers early onset mitochondrial dysfunction during adipogenesis of human liposarcoma SW872 cells [ Redox Biol, 2023, 67:102915] PubMed: 37866162
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
Neocortical Slow Oscillations Implicated in the Generation of Epileptic Spasms [ Ann Neurol, 2020, 10.1002/ana.25935] PubMed: 33068018
The evolution of a series of behavioral traits is associated with autism-risk genes in cavefish. [ BMC Evol Biol, 2018, 18(1):89] PubMed: 29909776
Pharmacokinetic Evaluation of Clozapine in Concomitant Use of Radix Rehmanniae, Fructus Schisandrae, Radix Bupleuri, or Fructus Gardeniae in Rats. [ Molecules, 2016, 21(6)] PubMed: 27240333
In Vitro Effects of Concomitant Use of Herbal Preparations on Cytochrome P450s Involved in Clozapine Metabolism [ Molecules, 2016, 21(5)597] PubMed: 27164071
Peony-Glycyrrhiza Decoction, an Herbal Preparation, Inhibits Clozapine Metabolism via Cytochrome P450s, but Not Flavin-Containing Monooxygenase in In Vitro Models. [Wang W, et al. Drug Metab Dispos, 2015, 43(7):1147-53] PubMed: 25948710

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。