CAS# 552292-08-7

Chemical Formula: C25H26F6N2O2

Exact Mass: 500.18985

Molecular Weight: 500.48

Elemental Analysis: C, 60.00; H, 5.24; F, 22.78; N, 5.60; O, 6.39

Description of rolapitant: Rolapitant, also known as SCH-619734, is a selective, bioavailable, CNS penetrant neurokinin NK1 receptor antagonist that shows behavioral effects in animals models of emesis. 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.