SCH-720881
SCH-720881 is the active metabolite of 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].
Product Specifications
CAS Number
2238886-63-8
UNSPSC
12352005
Target
Drug Metabolite; Neurokinin Receptor
Related Pathways
GPCR/G Protein; Metabolic Enzyme/Protease; Neuronal Signaling
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease
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(C[C@@H]4O)=O)CN2
Molecular Formula
C25H26F6N2O3
Molecular Weight
516.48
References & Citations
[1]Wang J, et al. Effects of rolapitant administered orally on the pharmacokinetics of dextromethorphan (CYP2D6), tolbutamide (CYP2C9), omeprazole (CYP2C19), efavirenz (CYP2B6), and repaglinide (CYP2C8) in healthy subjects. Support Care Cancer. 2019 Mar;27 (3) :819-827.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
NK1R
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