Fosaprepitant dimeglumine salt

- Overview
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    Background
    
    Fosaprepitant dimeglumine salt (L-758,298 MK-0517) is an antagonist of neurokinin-1[1].Fosaprepitant dimeglumine salt has shown the pharmacodynamic function by its active metabolite aprepitant. Fosaprepitanot dimeglumine salt has been found to be a highly selective antagonist of the NK-1 receptor and inhibit the cation of substance P. In addition, Fosaprepitant dimeglumine salt has been exhibited to have the effect on cisplatin induced emesis in the classical ferret model. Besides, because of the brain penetrating of aprepitant, Fosaprepitant dimeglumine salt has been revealed to have a very high affinity for the NK-1 receptor and increase the efficacy by dexamethasone, granisetron and so on. Fosaprepitant dimeglumine salt has been evaluated to use in the prevention of chemotherapy-induced nausea and vomiting (CINV) by combination with a 5-HT3 antagonist and a steroid [1].
    
    [1] Van Belle SJ1, Cocquyt V. Fosaprepitant dimeglumine (MK-0517 or L-785,298), an intravenous neurokinin-1 antagonist for the prevention of chemotherapy induced nausea and vomiting.Expert Opin Pharmacother. 2008 Dec; 9(18):3261-70.
- Properties
  - Categories
    
    Neurokinin-1 antagonist
    
    Alternative Name
    
    [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
    
    CAS Number
    
    265121-04-8
    
    Molecular Formula
    
    C37H56F7N6O16P
    
    Molecular Weight
    
    1004.83
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥50.24 mg/mL in DMSO; insoluble in EtOH; ≥13.16 mg/mL in H2O with ultrasonic
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CC(C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)OC2C(N(CCO2)CC3=NC(=O)N(N3)P(=O)(O)O)C4=CC=C(C=C4)F.CNCC(C(C(C(CO)O)O)O)O.CNCC(C(C(C(CO)O)O)O)O
    
    * For Research Use Only