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Fosaprepitant

Catalog No.
B1272
Neurokinin-1 antagonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$190.00
In stock
5mg
$97.00
In stock
10mg
$162.00
In stock
25mg
$323.00
In stock
50mg
$485.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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].

References:
[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt614.41
Cas No.172673-20-0
FormulaC23H22F7N4O6P
Solubility≥30.5mg/mL in DMSO
Chemical 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
SDFDownload SDF
Canonical SMILESCC(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
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Chemical structure

Fosaprepitant