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Casopitant mesylate (GW679769B) is a selective, brain-permeable, and orally active antagonist of the neurokinin 1 (NK1) receptor, and it is the second in its class of antiemetics.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,330 | 8-10 weeks | |
50 mg | $1,740 | 8-10 weeks | |
100 mg | $2,780 | 8-10 weeks |
Description | Casopitant mesylate (GW679769B) is a selective, brain-permeable, and orally active antagonist of the neurokinin 1 (NK1) receptor, and it is the second in its class of antiemetics. |
In vivo | In a ferret model of Cisplatin-induced emesis, Casopitant inhibits retching and vomiting and reduces nausea-like behaviors in a dose-dependent manner. Following a single intraperitoneal dose, radioactive labeled Casopitant ([14C]Casopitant) is rapidly absorbed, with plasma and brain concentrations being approximately equal at two hours post-dosing. [14C]Casopitant is found in the brain as the parent compound and two major oxidative metabolites (M1 and M2), accounting for approximately 76%, 19%, and 3% of the radioactivity, respectively. Casopitant exhibits high affinity for brain NK1 receptors in the ferret [2]. |
Alias | GW679769B |
Molecular Weight | 712.72 |
Formula | C31H39F7N4O5S |
Cas No. | 414910-30-8 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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