Shelf life (days): 1460.0
Formulation: A solid
Formal Name: (2R,4S)-4-(4-acetyl-1-piperazinyl)-N-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl]-2-(4-fluoro-2-methylphenyl)-N-methyl-1-piperidinecarboxamide, methanesulfonate
Purity: ≥98%
Formula Markup: C30H35F7N4O2 / CH3SO3H
Formula Weight: 712.724822
CAS Number: 414910-30-8
Notes: An NK1 receptor antagonist (Ki = 0.33 nM); selective for the NK1 receptor over a panel of 70 GPCRs, ion channels, and transporters at 10 µM; inhibits substance P-induced increases in intracellular calcium in CHO cells expressing the human NK1 receptor (pA2 = 9.7); increases social interaction time in gerbils, indicating anxiolytic-like activity, at 1 mg/kg; inhibits GR73632-induced foot tapping in gerbils (ID50s = 0.08, 0.04, 0.19, and 1.1 mg/kg at 1, 4, 8, or 24 hours prior to GR73632, respectively)