Casopitant (mesylate)
Product Specifications
UNSPSC Description
Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of substance P. Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV)[1][2].
Target Antigen
Cytochrome P450; Neurokinin Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein;Metabolic Enzyme/Protease;Neuronal Signaling
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease; Cancer
Assay Protocol
https://www.medchemexpress.com/casopitant-mesylate.html
Solubility
DMSO : 33.33 mg/mL (ultrasonic;warming;heat to 60°C)
Smiles
O=C(N1[C@@H](C2=CC=C(F)C=C2C)C[C@@H](N3CCN(C(C)=O)CC3)CC1)N([C@@H](C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)C)C.CS(=O)(O)=O
Molecular Weight
712.72
References & Citations
[1]Ruhlmann C, et al. Casopitant: a novel NK(1)-receptor antagonist in the prevention of chemotherapy-induced nausea and vomiting. Ther Clin Risk Manag. 2009 Apr;5(2):375-84.|[2]Minthorn E, et al. Pharmacokinetics and brain penetration of casopitant, a potent and selective neurokinin-1 receptor antagonist, in the ferret. Drug Metab Dispos. 2008 Sep;36(9):1846-52.
Shipping Conditions
Room Temperature
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-14405A/Casopitant-mesylate-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-14405A/Casopitant-mesylate-SDS-MedChemExpress.pdf
Clinical Information
Phase 3
CAS Number
414910-30-8
Available Sizes
Curated Selection
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