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    Miltefosine (Impavido; HePC)
    Miltefosine (Impavido; HePC)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0166
    CAS #: 58066-85-6Purity ≥98%

    Description: Miltefosine (Impavido; HePC), an alkyl-phosphocholine compound, is a potent, orally- and topically-bioactive, broad spectrum antimicrobial and anti-leishmanial medication that also has potential antineoplastic activity. It acts by inhibiting PI3K/Akt with an ED50 of 17.2 μM and 8.1 μM in carcinoma cell lines A431 and HeLa.

    References:  Br J Cancer. 2001 May 18;84(10):1405-11.

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    • 香港大学
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    Molecular Weight (MW)407.57
    FormulaC21H46NO4P
    CAS No.58066-85-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: <1 mg/mL
    Water: 82 mg/mL (201.2 mM)
    Ethanol: 82 mg/mL (201.2 mM)
    Solubility (In vivo)Saline: 30mg/mL
    Other info

    Synonym: HePC; Hexadecyl phosphocholine; Miltefosin C; HePC; Hexadecylphosphocholine; HDPC; Hexadecylphosphorylcholine; Miltefosinum; mpavido; Miltex; Choline Phosphate Hexadecyl Ester Hydroxide Inner Salt; hexadecylphosphocholine; Miltefosin; Miltefosina; Miltefosinum

    Chemical Name: hexadecyl (2-(trimethylammonio)ethyl) phosphate

    InChi Key: PQLXHQMOHUQAKB-UHFFFAOYSA-N

    InChi Code: InChI=1S/C21H46NO4P/c1-5-6-7-8-9-10-11-12-13-14-15-16-17-18-20-25-27(23,24)26-21-19-22(2,3)4/h5-21H2,1-4H3

    SMILES Code: O=P(OCCCCCCCCCCCCCCCC)([O-])OCC[N+](C)(C)C


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    In Vitro

    Kinase Assay:

    Cell Assay: 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.

    Miltefosine is an alkylphosphocholine drug with demonstrated activity against various parasite species and cancer cells as well as some pathogenic bacteria and fungi. Miltefosine inhibits PKC from NIH3T3 cells in cell-free extracts with a IC50 of about 7 μM. Miltefosine targets HIV infected macrophages, which play a role in vivo as long-lived HIV-1 reservoirs. Miltefosine acts by inhibiting the PI3K/Akt pathway, thus removing the infected macrophages from circulation, without affecting healthy cells. Miltefosine inhibits the PI3K/Akt survival pathway in carcinoma cell lines. Miltefosine causes skeletal muscle insulin resistance in vitro by interfering with the insulinsignalling pathway and inhibiting insulin-stimulated glucose uptake. Miltefosine inhibits insulin-stimulated Akt phosphorylation in a dose-dependent manner with 75% inhibition at 40 μM and 98% inhibition at 60 μM.

    In Vivo

    Miltefosine inhibits anti-IgE induced histamine release from human skin mast cells. Miltefosine can reduce cytokines IL-1β, IL-4, and IL-6 in certain skin tissue cells and also strongly impede the esterification of cholesterol

    Animal model

    BC-1 cells xenografted NOD-SCID mice

    Formulation & Dosage

    Formulated inPBS; 50 mg/kg; i.p.

    References

    [1] Meuillet EJ, et al. Mol Cancer Ther, 2010, 9(3), 706-717.

     


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Miltefosine

    Treatment of HIV-infected macrophages with PI3K/Akt inhibitors reduces HIV-1 production and induces cell death. Retrovirology, 2008, 5, 11.

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