Rolapitant

Rolapitant

• CAS Number: 552292-08-7
• UNSPSC Description: Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model[1][2].
• Target Antigen: Neurokinin Receptor
• Type: Reference compound
• Related Pathways: GPCR/G Protein;Neuronal Signaling
• Applications: Cancer-programmed cell death
• Field of Research: Cancer; Neurological Disease
• Assay Protocol: https://www.medchemexpress.com/Rolapitant.html
• Solubility: DMSO : ≥ 30 mg/mL
• Smiles: C[C@@](C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)([H])OC[C@@]2(C3=CC=CC=C3)CC[C@@](CCC4=O)(N4)CN2
• Molecular Weight: 500.48
• References & Citations: [1]Duffy RA, et al. Rolapitant (SCH 619734): a potent, selective and orally active neurokininNK1 receptor antagonist with centrally-mediated antiemetic effects inferrets. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100.|[2]Rapoport B, et al. Study of rolapitant, a novel, long-acting, NK-1 receptor antagonist, for the prevention of chemotherapy-induced nausea and vomiting (CINV) due to highly emetogenic chemotherapy (HEC). Support Care Cancer. 2015 Nov;23(11):3281-8.
• Shipping Conditions: Room Temperature
• Clinical Information: Launched