Casopitant (mesylate)

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 (HY-P0201) . 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].

Product Specifications

CAS Number

[414910-30-8]

Product Name Alternative

GW679769B

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

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

Purity

99.83

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 Formula

C31H39F7N4O5S

Molecular Weight

712.72

Precautions

H302, H315, H319, H335

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.