Aprepitant | NK-1 antagonist

CAS:
170729-80-3
Catalog Number:
10-4366
Activity:
NK-1 antagonist
Chemical Names:
3-[[(2R,3S)-2-[(1R)-1-bis(Trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-1,4dihydro-1,2,4-triazol-5-one
Alternate Name:
MK-0869
Molecular Weight:
534.43
Molecular Formula:
C23H21F7N4O3
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
10 mg$40.00
50 mg$130.00

Aprepitant (170729-80-3) is a potent human neurokinin-1 (NK-1) antagonist.1  It is an FDA approved medication for the treatment of chemotherapy-induced and postoperative nausea and vomiting.2 Aprepitant is also a selective activator of the K2P channel TRAAK.3 It also has been shown to have multiple anticancer effects.4

References/Citations:

  1. Hale et al. (1998), Structural optimization affording 2-(R)-(1-(R)-3,5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1receptor antagonist; Med. Chem. 41 4607
  2. Rapoport and Smit (2017); Clinical pharmacology of neurokinin-1 receptor antagonists for the treatment of nausea and vomiting associated with chemotherapy, Expert Opin. Drug Saf., 16 697
  3. McCoull et al. (2022); Aprepitant is a novel, selective activator of the K2P channel TRAAK, Biochem. Biophys. Res. Commun., 588 41
  4. Muñoz and Coveñas (2020); The Neurokinin-1 Receptor Antagonist Aprepitant: An Intelligent Bullet against Cancer?, Cancer (Basel), 12 2682
CAS:
170729-80-3
Catalog Number:
10-4366
Activity:
NK-1 antagonist
Chemical Names:
3-[[(2R,3S)-2-[(1R)-1-bis(Trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-1,4dihydro-1,2,4-triazol-5-one
Alternate Name:
MK-0869
Molecular Weight:
534.43
Molecular Formula:
C23H21F7N4O3
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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