Miltefosine

製品コードS3056 バッチS305603

印刷

化学情報

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

C21H46NO4P
分子量 407.57 CAS No. 58066-85-6
Solubility (25°C)* 体外 Water 82 mg/mL (201.19 mM)
Ethanol 82 mg/mL (201.19 mM)
DMSO Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
Saline

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。

 30.000mg/ml (73.61mM) Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, 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 Miltefosine (Hexadecylphosphocholine) inhibits PI3K/Akt activity with ED50 of 17.2 μM and 8.1 μM in carcinoma cell lines A431 and HeLa, first oral drug for Visceral leishmaniasis, effective against both promastigotes and amastigotes.
in vitro Miltefosine is an alkylphosphocholine drug with demonstrated activity against various parasite species and cancer cells as well as some pathogenic bacteria and fungi. This compound inhibits PKC from NIH3T3 cells in cell-free extracts with a IC50 of about 7 μM.[1] It targets HIV infected macrophages, which play a role in vivo as long-lived HIV-1 reservoirs. This chemical acts by inhibiting the PI3K/Akt pathway, thus removing the infected macrophages from circulation, without affecting healthy cells.[2] It inhibits the PI3K/Akt survival pathway in carcinoma cell lines.[3] This compound causes skeletal muscle insulin resistance in vitro by interfering with the insulinsignalling pathway and inhibiting insulin-stimulated glucose uptake. It inhibits insulin-stimulated Akt phosphorylation in a dose-dependent manner with 75% inhibition at 40 μM and 98% inhibition at 60 μM.[4]
in vivo Miltefosine inhibits anti-IgE induced histamine release from human skin mast cells. This compound can reduce cytokines IL-1β, IL-4, and IL-6 in certain skin tissue cells and also strongly impede the esterification of cholesterol. [5]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 BCLM, VG-1, BC-1, and BCBL-1 PEL cell lines
濃度 10, 20, 30, 40, and 50μM
反応時間 3 days
実験の流れ 2 × 105 PEL cells are treated with the therapeutic compounds at the indicated doses or with appropriate vehicle as a negative control. Cells are followed for 96 hours, and cell viability is determined by trypan blue exclusion performed in quadruplicate.
動物実験 動物モデル BC-1 cells xenografted NOD-SCID mice
投薬量 50 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/1846318/
  • https://pubmed.ncbi.nlm.nih.gov/18237430/
  • https://pubmed.ncbi.nlm.nih.gov/12569304/
  • https://pubmed.ncbi.nlm.nih.gov/16752184/
  • https://pubmed.ncbi.nlm.nih.gov/19917276/
  • https://pubmed.ncbi.nlm.nih.gov/20299510/

カスタマーフィードバック

, , Biochem Biophys Res Commun, 2016, 469(4):1034-40.

, , Biochem Biophys Res Commun, 2016, 469(4):1034-40.

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：

Anti-TNBC effects of Lappaol F by targeting epithelial-mesenchymal transition via regulation of GSK-3β/YAP/β-catenin and PI3K/AKT pathways [ Front Pharmacol, 2025, 16:1496511] PubMed: 39989901
Low-Dose Perifosine, a Phase II Phospholipid Akt Inhibitor, Selectively Sensitizes Drug-Resistant ABCB1-Overexpressing Cancer Cells [ Biomol Ther (Seoul), 2025, 33(1):170-181] PubMed: 39632683
Formulation, in vitro evaluation and therapeutic effect of chitosan coated pluronic F127 micelles containing miltefosine for the treatment of visceral leishmaniasis in domestic dogs naturally infected by Leishmania infantum [ Res Vet Sci, 2025, 182:105467] PubMed: 39591859
Miltefosine Induces Reproductive Toxicity During Sperm Capacitation by Altering PI3K/AKT Signaling Pathway [ Environ Toxicol Pharmacol, 2024, S1382-6689(24)00205-9] PubMed: 39265707
Chitosan nanoparticles improve the effectivity of miltefosine against Acanthamoeba [ PLoS Negl Trop Dis, 2024, 18(3):e0011976] PubMed: 38527059
FAT10 Combined with Miltefosine Inhibits Mitochondrial Apoptosis and Energy Metabolism in Hypoxia-Induced H9C2 Cells by Regulating the PI3K/AKT Signaling Pathway [ Evid Based Complement Alternat Med, 2022, 2022:4388919] PubMed: 36034957
Bioanalytical methods for pharmacokinetic studies of antileishmanial drugs [ Biomed Chromatogr, 2022, e5519.] PubMed: 36208186
FOXM1-mediated activation of phospholipase D1 promotes lipid droplet accumulation and reduces ROS to support paclitaxel resistance in metastatic cancer cells [ Free Radic Biol Med, 2021, S0891-5849(21)00821-2] PubMed: 34808333
CORO1C is Associated With Poor Prognosis and Promotes Metastasis Through PI3K/AKT Pathway in Colorectal Cancer [ Front Mol Biosci, 2021, 8:682594] PubMed: 34179087
The PI3K/mTOR dual inhibitor GSK458 potently impedes ovarian cancer tumorigenesis and metastasis. [ Cell Oncol (Dordr), 2020, 8] PubMed: 32382996

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。