Formulation: A solid
Formal Name: 5-((2-(1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl-2,3,5,6-d4)morpholino)methyl)-2,4-dihydro-3H-1,2,4-triazol-3-one
Purity: ≥99% deuterated forms (d1-d4)
Formula Markup: C23H17D4F7N4O3
Formula Weight: 538,5
Shelf life (days): 1460
CAS Number: 2748471-42-1
Notes: rac-Aprepitant-d4 is intended for use as an internal standard for the quantification of aprepitant (Item No. 14867) by GC- or LC-MS. Aprepitant an antiemetic compound and antagonist of the neurokinin-1 (NK1) receptor (Ki = 3 nM; IC50 = 0.09 nM for the human receptor).{24162,24160} It is selective for NK1 over NK3 receptors (Ki = 454.1 nM for human NK3).{24162} In vivo, aprepitant (1 mg/kg) prevents plasma extravasation into the esophagus of guinea pigs induced by substance P (Item No. 24035).{24161} It also reduces NK1-agonist-induced foot tapping in gerbils. Formulations containing aprepitant have been used to prevent chemotherapy-induced nausea and vomiting.
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