An antiemetic and NK1 antagonist (Ki = 3 nM; IC50 = 0.09 nM for the human receptor); selective for NK1 over NK3 receptors (Ki = 454.1 nM for human NK3); prevents substance P-induced plasma extravasation into the esophagus of guinea pigs at 1 mg/kg; reduces NK1-agonist-induced foot tapping in gerbils

Aprepitant – 1 mg

Brand:
Cayman
CAS:
170729-80-3
Storage:
-20
UN-No:
Non-Hazardous - /

Aprepitant an antiemetic 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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Description

An antiemetic and NK1 antagonist (Ki = 3 nM; IC50 = 0.09 nM for the human receptor); selective for NK1 over NK3 receptors (Ki = 454.1 nM for human NK3); prevents substance P-induced plasma extravasation into the esophagus of guinea pigs at 1 mg/kg; reduces NK1-agonist-induced foot tapping in gerbils

Formal name: 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

Synonyms:  Emend|L-754,030|MK-869|ONO-7436

Molecular weight: 534.4

CAS: 170729-80-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Pain Research

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