Rolapitant

  • Chemical Properties
CAS No. 552292-08-7 Cat. No. BCP09609
Name Rolapitant
Synonyms (5S,8S)-8-[[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]methyl]-8-phenyl-1,9-diazaspiro[4.5]decan-2-one;
Formula C25H26F6N2O2 M. Wt 500.48
  • Biological Activity
Description . In vitro studies indicate that rolapitant has a high affinity for the human NK1 receptor of 0.66 nM and high selectivity over the human NK2 and NK3 subtypes of >1000-fold. Rolapitant is a functionally competitive antagonist, as measured by calcium efflux, with a calculated Kb of 0.17 nM.
Pathways GPCR/G Protein 
Targets NK Receptor 

Structure

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