Rolapitant (hydrochloride)

Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride does not interact with CYP3A4. Rolapitant hydrochloride shows potent anti-emetic activity in a ferret emesis model[1][2].

Product Specifications

CAS Number

[858102-79-1]

Product Name Alternative

SCH619734 (hydrochloride)

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

Neurokinin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/rolapitant-hydrochloride.html

Solubility

10 mM in DMSO

Smiles

O=C1N[C@]2(CN[C@@](C3=CC=CC=C3)(CO[C@@H](C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)C)CC2)CC1.[H]Cl

Molecular Formula

C25H27ClF6N2O2

Molecular Weight

536.94

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

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.