Rolapitant (hydrochloride)
Product Specifications
UNSPSC Description
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].
Target Antigen
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 Weight
536.94
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
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-14751A/Rolapitant-hydrochloride-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-14751A/
Clinical Information
Launched
CAS Number
858102-79-1
Curated Selection
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