Fluvoxamine (DU-23000) maleate

製品コードS1336 バッチS133603

印刷

化学情報

 Chemical Structure Synonyms MK-264,DU-23000 maleate Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C19H25F3N2O6

分子量 434.41 CAS No. 61718-82-9
Solubility (25°C)* 体外 DMSO 86 mg/mL (197.96 mM)
Ethanol 86 mg/mL (197.96 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 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。

4.300mg/ml (9.90mM) Taking the 1 mL working solution as an example, add 50 μL of 86 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. 
Clear solution
5% DMSO 95% 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。

4.300mg/ml (9.90mM) Taking the 1 mL working solution as an example, add 50 μL of 86 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. 
* <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 Fluvoxamine maleate (DU-23000, MK-264) is a selective serotonin (5-HT) reuptake inhibitor (SSRI), used in the treatment of obsessive-compulsive disorder.
in vitro Fluvoxamine increases [5-HT]ex levels in rat the prefrontal cortex and thalamus, and also increases [DA]ex levels in the striatum. [1] Fluvoxamine maleate ameliorates tactile allodynia via spinal 5-HT2A/2C receptors, by acting on the receptors or 5-HT neurons. [2]
in vivo Fluvoxamine maleate also exhibits the antinociception in a dose-dependent manner in the paw pressure test in non-ligated mice. Fluvoxamine maleate also induces antinociceptive effect in the acute paw pressure test, and this effect is antagonized by the 5-HT3 receptor antagonist granisetron. [2] Fluvoxamine (10 and 30 mg/kg, i.p.) enhances synaptic efficacy in the hippocampo-mPFC pathway in a dose-dependent manner in the rat hippocampo-medial prefrontal cortex (mPFC). [3] Fluvoxamine (10 and 30 mg/kg, i.p.) suppresses long-term potentiation (LTP) in the hippocampal CA1 field of anesthetized rats. Fluvoxamine (30 mg/kg, i.p.)-induced suppression of LTP is completely reversed by the 5-HT(1A) receptor antagonist NAN-190 (0.5 mg/kg, i.p), but not by the 5-HT(4) receptor antagonist GR 113808 (20 mg/rat, i.c.v.) and the 5-HT(7) receptor antagonist DR 4004 (10 mg/rat, i.c.v.). [4] Fluvoxamine maleate reinforces the response to norepinephrine of isolated rat vas deferens incubated in Krebs-Henseleit solution. Fluvoxamine maleate and Fluoxetine hydrochloride inhibit the contraction induced by potassium ion on the isolated rat uterus preparation with IC50 of 3.99μM and 18.2μM, respectively. [5]

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/15138756/
  • https://pubmed.ncbi.nlm.nih.gov/16846619/
  • https://pubmed.ncbi.nlm.nih.gov/12213308/
  • https://pubmed.ncbi.nlm.nih.gov/12480170/
  • https://pubmed.ncbi.nlm.nih.gov/9147017/

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 amiodarone for bladder cancer treatment [ Cancer Res Commun, 2025, 10.1158/2767-9764.CRC-24-0433] PubMed: 40353763
SSRI antidepressant citalopram reverses the Warburg effect to inhibit hepatocellular carcinoma by directly targeting GLUT1 [ Cell Rep, 2024, 43(10):114818] PubMed: 39388353
Activation of the sigma-1 receptor ameliorates neuronal ferroptosis via IRE1α after spinal cord injury [ Brain Res, 2024, 1838:149011] PubMed: 38763502
Predicting Clinical Outcomes of SARS-CoV-2 Drug Efficacy with a High-Throughput Human Airway Microphysiological System [ Adv Biol (Weinh), 2024, e2300511.] PubMed: 39123296
A human primary airway microphysiological system infected with SARS-CoV-2 distinguishes the treatment efficacy between nirmatrelvir and repurposed compounds [ bioRxiv, 2023, 10.1101/2023.06.27.546790] PubMed: None
A temperature-regulated circuit for feeding behavior [ Nat Commun, 2022, 13(1):4229] PubMed: 35869064
A temperature-regulated circuit for feeding behavior [ Nat Commun, 2022, 13(1):4229] PubMed: 35869064
JIB-04 Has Broad-Spectrum Antiviral Activity and Inhibits SARS-CoV-2 Replication and Coronavirus Pathogenesis [ mBio, 2022, 13(1):e0337721] PubMed: 35038906
Fluvoxamine confers neuroprotection via inhibiting infiltration of peripheral leukocytes and M1 polarization of microglia/macrophages in a mouse model of traumatic brain injury [ J Neurotrauma, 2022, 10.1089/neu.2021.0355] PubMed: 35502478
A temperature-regulated circuit for feeding behavior [ Research Square, 2021, 10.21203/rs.3.rs-916525/v1] PubMed: None

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。