- Product NameRolapitant
- Brief DescriptionInhibitors
- Purification98.00%
- Biological ActivityRolapitant, also known as SCH-619734, is an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic Y chemotherapy. Compared to other NK1-receptor antagonists, rolapitant has both a more rapid onset of action and a much longer half-life. Rolapitant was approved in 2015. Rolapitant hydrochloride is approved to be used with other drugs to prevent: Nausea and vomiting caused by chemotherapy.
- Target NameNeurokinin 1 antagonist
- CAS No. 552292-08-7
- Calculated MW 500.48
- Formulation C25H26F6N2O2
- Storage 3 years -20˚C powder;2 years -80˚C in solvent;