Ivermectin

製品コードS1351 バッチS135102

印刷

化学情報

Chemical Structure Synonyms MK-933 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C48H74O14
分子量 875.09 CAS No. 70288-86-7
Solubility (25°C)* 体外 DMSO 175 mg/mL (199.97 mM)
Ethanol 28 mg/mL (31.99 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.
* <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.

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生物活性

製品説明 Ivermectinは、広範囲スペクトルの抗寄生虫薬として使用される、グルタミン酸作動性塩化物チャネル(GluCls)活性化因子です。Ivermectin (MK-933, IVM)は、P2X4およびα7ニコチン性アセチルコリン受容体（nAChRs）の特異的なポジティブアロステリックエフェクターです。Ivermectin (MK-933)は、Impα/β1を介した核内輸送の特異的阻害剤であり、HIV-1およびデングウイルスの両方に対して強力な抗ウイルス活性を有します。Ivermectinは、AKT/mTORシグナル伝達経路を介してオートファジーを誘導し、マイトファジーを誘導します。
in vitro

Ivermectin has potent antiviral activity towards both HIV-1 anddengue virus, both of which are strongly reliant on importin α/β nuclear import, with respect to the HIV-1 integrase and NS5 (non-structural protein 5) polymerase proteins respectively. This compound binds to a novel site on the GABAA receptor and allosterically enhances the affinity of the GABA binding site in mouse hippocampal embryonic neurons. It disrupts neurotransmission processes regulated by GluCl activity by binding to nematode glutamate-gated chloride channels (GluCls). This chemical decreases the amount of protein released from microfilariae.

in vivo

Ivermectin (1.25-10 mg/kg, intraperitoneal) significantly reduces 24-h alcohol consumption and intermittent limited access (4-hours) binge drinking, and operant alcohol self-administration (1-h). This compound also produces a significant reduction in 24-h saccharin consumption, but does not alter operant sucrose self-administration. It improves mouse survival rate induced by a lethal dose of LPS. This chemical significantly decreases the production of TNF-alpha, IL-1ss and IL-6 in vivo and in vitro. It suppresses NF-kB translocation induced by LPS.

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/22417684/
  • https://pubmed.ncbi.nlm.nih.gov/9770244/
  • https://pubmed.ncbi.nlm.nih.gov/21041637/
  • https://pubmed.ncbi.nlm.nih.gov/22465817/
  • https://pubmed.ncbi.nlm.nih.gov/19109745/
  • https://pubmed.ncbi.nlm.nih.gov/20463059/

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：

Nucleus-translocated glucokinase functions as a protein kinase to phosphorylate TAZ and promote tumour growth [ Nat Commun, 2025, 16(1):7156] PubMed: 40759645
The aryl hydrocarbon receptor inhibits antigen presentation to promote progression of pancreatic ductal adenocarcinoma [ J Adv Res, 2025, S2090-1232(25)00874-4] PubMed: 41203070
Anti-cancer small-molecule Inauhzin-C confines its cytotoxicity to cancer cells by targeting GRP78 [ Biomed Pharmacother, 2025, 189:118248] PubMed: 40561593
N4BP1 is a nucleocytoplasmic shuttling protein and recognizes aggregates of the ubiquitin-like protein NEDD8 to protect cells under heat shock [ J Biol Chem, 2025, 301(9):110511] PubMed: 40701250
Avermectins Inhibit Replication of Parvovirus B19 by Disrupting the Interaction Between Importin α and Non-Structural Protein 1 [ Viruses, 2025, 17(2)220] PubMed: 40006975
Nuclear PD-L1 compartmentalization suppresses tumorigenesis and overcomes immunocheckpoint therapy resistance in mice via histone macroH2A1 [ J Clin Invest, 2024, 134(22)e181314] PubMed: 39545415
The Dual-Targeted Fusion Inhibitor Clofazimine Binds to the S2 Segment of the SARS-CoV-2 Spike Protein [ Viruses, 2024, 16(4)640] PubMed: 38675980
Ivermectin Strengthens Paclitaxel Effectiveness in High-Grade Serous Carcinoma in 3D Cell Cultures [ Pharmaceuticals (Basel), 2024, 18(1)14] PubMed: 39861076
The CHARGE syndrome-associated protein FAM172A controls AGO2 nuclear import [ Life Sci Alliance, 2023, 6(8)e202302133] PubMed: 37221016
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization [ Cell Rep Methods, 2023, 3(10):100599] PubMed: 37797618

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。