Aprepitant

RT

534, 43

White to off-white powder

Aprepitant an antiemetic and antagonist of the neurokinin-1 (NK1) receptor (Ki = 3nM; IC50 = 0.09nM for the human receptor).It is selective for NK1 over NK3 receptors (Ki = 454.1nM for human NK3). In vivo, aprepitant (1mg/Kg) prevents plasma extravasation into the esophagus of guinea pigs induced by substance P. It also reduces NK1-agonist-induced foot tapping in gerbils. Formulations containing aprepitant have been used to prevent chemotherapy-induced nausea and vomiting.

Synonyms:
5-[[(2R, 3S)-2-[(1R)-1-[3, 5-Bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1, 2-dihydro-3H-1, 2, 4-triazol-3-one; Emend; L 754030; MK-869; ONO-7436

CAS Number:
170729-80-3

Molecular Formula:
C23H21F7N4O3

Molecular Weight:
534.43

Appearance:
White to off-white powder

Purity:
≥98%

Identity (1H NMR):
Conforms to structure

Melting Point:
As Reported

Storage and Stability:
Store at RT. Stable for 6 months after receipt.

Important Note:
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.

Toxicity and Hazards: 
All products should be handled by qualified personnel only, trained in laboratory procedures.