Fosaprepitant

Name: Fosaprepitant
Price: 364.00 USD

Catalog Number:

L002369897APE

Mfr. No.:

APE-B1272

Price:

$364

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- Overview
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    Background
    
    Fosaprepitant (L-758,298 MK-0517) is an antagonist of neurokinin-1[1].Fosaprepitant has shown the pharmacodynamic function by its active metabolite aprepitant. Fosaprepitanot has been found to be a highly selective antagonist of the NK-1 receptor and inhibit the cation of substance P. In addition, Fosaprepitant 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 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 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
    
    CAS Number
    
    172673-20-0
    
    Molecular Formula
    
    C23H22F7N4O6P
    
    Molecular Weight
    
    614.41
    
    Appearance
    
    A solid
    
    Purity
    
    99.22%
    
    Solubility
    
    ≥30.5 mg/mL in DMSO; insoluble in H2O; ≥22.13 mg/mL in EtOH 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
    
    * For Research Use Only