Ivermectin

製品コードS1351 バッチS135101

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
* <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 is a glutamate-gated chloride channel (GluCls) activator, used as a broad-spectrum antiparasitic drug. Ivermectin (MK-933, IVM) is a specific positive allosteric effector of P2X4 and α7 nicotinic acetylcholine receptors (nAChRs). Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. Ivermectin induces autophagy through the AKT/mTOR signaling pathway and mitophagy.
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. [1] Ivermectin binds to a novel site on the GABAA receptor and allosterically enhances the affinity of the GABA binding site in mouse hippocampal embryonic neurons. [2] Ivermectin disrupts neurotransmission processes regulated by GluCl activity by binding to nematode glutamate-gated chloride channels (GluCls). Ivermectin decreases the amount of protein released from microfilariae. [3]

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). Ivermectin also produces a significant reduction in 24-h saccharin consumption, but does not alter operant sucrose self-administration. [4] Ivermectin improves mouse survival rate induced by a lethal dose of LPS. Ivermectin significantly decreases the production of TNF-alpha, IL-1ss and IL-6 in vivo and in vitro. Ivermectin suppresses NF-kB translocation induced by LPS. [5]

プロトコル(参考用のみ)

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:

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
Ivermectin and gemcitabine combination treatment induces apoptosis of pancreatic cancer cells via mitochondrial dysfunction [ Front Pharmacol, 2022, 13:934746] PubMed: 36091811
The Antineoplastic Effect of Carboplatin Is Potentiated by Combination with Pitavastatin or Metformin in a Chemoresistant High-Grade Serous Carcinoma Cell Line [ Int J Mol Sci, 2022, 24(1)97] PubMed: 36613537
Pitavastatin and Ivermectin Enhance the Efficacy of Paclitaxel in Chemoresistant High-Grade Serous Carcinoma [ Cancers (Basel), 2022, 14(18)4357] PubMed: 36139522
Synergistic drug combinations designed to fully suppress SARS-CoV-2 in the lung of COVID-19 patients [ PLoS One, 2022, 17(11):e0276751] PubMed: 36355808
Repurposing Ivermectin to augment chemotherapy's efficacy in osteosarcoma [ Hum Exp Toxicol, 2022, 41:9603271221143693] PubMed: 36503300
Nucleocytoplasmic Shuttling of Porcine Parvovirus NS1 Protein Mediated by the CRM1 Nuclear Export Pathway and the Importin α/β Nuclear Import Pathway [ J Virol, 2021, JVI0148121] PubMed: 34643426
Ivermectin induces apoptosis of esophageal squamous cell carcinoma via mitochondrial pathway [ BMC Cancer, 2021, 21(1):1307] PubMed: 34876051
[ Nat Cell Biol, 2020, ] PubMed: 32839551

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。