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Fosaprepitant dimeglumine

  • Post Date:

    Jun 06,2020
  • Expiry Date:

    Jun 06,2021
  • Detailed Description:

    Cas No. :265121-04-8 Quantity: 1Metric Tons
    Specs:99%min
    Product Name: Fosaprepitant dimeglumine
    Synonyms: Fosaprepitant-d4 Dimeglumine;[5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-3-oxo-1H-1,2,4-triazol-2-yl]phosphonic acid,(2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentol;D-Glucitol, 1-deoxy-1-(methylamino)-, (3-(((2R,3S)-2-((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)-4- morpholinyl)methyl)-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl)phosphonate (2:1) (salt);Mk-0517;Fosaprepitant dimeglumine(MK-0517);Fosaprepitant dimeglumine(MK0517,Emend, Inemend);Phosphonic acid, (3-(((2R,3S)-2-((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)-4-morpholinyl)methyl)-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl)-, compd. with 1-deoxy-1-(methylamino)-D-glucitol (1:2);Unii-D35fm8T64x
    CAS: 265121-04-8
    MF: C60H78F14N10O20P2
    MW: 1587.2414868
    EINECS: 682-419-4
    Product Categories: Other APIs;Inhibitors
    Mol File: 265121-04-8.mol
    Fosaprepitant dimeglumine Structure
    Fosaprepitant dimeglumine Chemical Properties
    Safety Information
    MSDS Information
    Fosaprepitant dimeglumine Usage And Synthesis
    Description One of the most debilitating side effects of cancer treatment is CINV. Although concomitant anti-emetic agents have been prevalent for the past two decades, 50 60% of patients are still plagued by CINV. To meet this need, fosaprepitant dimeglumine has been launched as a water-soluble, phosphoryl pro-drug of aprepitant for intravenous applications. This pro-drug is rapidly converted to aprepitant in vivo, which has a high affinity for the NK-1 receptor (IC50= 90 50 pM for the displacement of [125I]-substance P from hNK-1 expressed in CHO cells); antagonism 606 Shridhar Hegde and Michelle Schmidt of NK-1 prevents binding of the endogenous substance P that is known to induce vomiting. Fosaprepitant is prepared by the regioselective phosphorylation of aprepitant with dibenzylphosphoryl chloride followed by catalytic hydrogenolysis in the presence of N-methyl-Dglucamine. It is approved for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly and moderately emetogenic cancer chemotherapy.
    Originator Merck (United States)
    Uses Fosaprepitant is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist
    Definition ChEBI: An organoammonium salt obtained by reaction of fosaprepitant with two equivalents of 1-deoxy-1-(methylamino)-D-glucitol. A substance P/neurokinin 1 (NK1) receptor antagonist. Aprepitant is a selective high-affinity antagonist of human subs ance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting and postoperative nausea and vomiting
    Brand name IvEmend
  • CAS Registry Number:

    265121-04-8
  • Synonyms:

    ;Fosaprepitant dimeglumine [USAN];Ivemend;MK-0517;UNII-D35FM8T64X;D-Glucitol, 1-deoxy-1-(methylamino)-, (3-(((2R,3S)-2-((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)-4- morpholinyl)methyl)-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl)phosphonate (2:1) (salt);Phosphonic acid, (3-(((2R,3S)-2-((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)-4-morpholinyl)methyl)-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl)-, compd. with 1-deoxy-1-(methylamino)-D-glucitol (1:2);1-Deoxy-1-(Methylamino)-D-Glucitol [3-[[(2R,3S)-2-[(1R)-1-[3,5-Bis(Trifluoromethyl)Phenyl]Ethoxy]-3-(4-Fluorophenyl)-4-Morpholinyl]Methyl]-2,5-Dihydro-5-Oxo-1H-1,2,4-Triazol-1-Yl]Phosphonate;Fosapitant Dimeglumine;
  • Molecular Formula:

    C23H22F7N4O6P·2C7H17NO<
  • Molecular Weight:

    1004.8354
  • Molecular Structure:

    265121-04-8 Fosaprepitant Dimeglumine
  • Company:

    shanghai missyou chemical co.,ltd.         
  • Contact:

    eileen zhang
  • Tel:

    +86-18101936766
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    021-58583907
  • Email:

    eileen@shmychem.com
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