Rolapitant

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].

Product Specifications

CAS Number

[552292-08-7]

Product Name Alternative

SCH619734

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

Neurokinin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Cancer-programmed cell death

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Rolapitant.html

Purity

99.89

Solubility

DMSO : ≥ 30 mg/mL

Smiles

C[C@H](C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)OC[C@@]2(C3=CC=CC=C3)CC[C@@]4(NC(CC4)=O)CN2

Molecular Formula

C25H26F6N2O2

Molecular Weight

500.48

Precautions

H315, H319, H320

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.