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Casopitant mesylate (GW679769B) is a selective, brain permeable, and orally active antagonist of neurokinin 1 (NK1) receptor. It is a second in the class of antiemetics.
Casopitant mesylate (GW679769B) is a selective, brain permeable, and orally active antagonist of neurokinin 1 (NK1) receptor. It is a second in the class of antiemetics.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 12,700 | 8-10周 | |
50 mg | ¥ 16,600 | 8-10周 | |
100 mg | ¥ 21,500 | 8-10周 |
产品描述 | Casopitant mesylate (GW679769B) is a selective, brain permeable, and orally active antagonist of neurokinin 1 (NK1) receptor. It is a second in the class of antiemetics. |
体内活性 | In a ferret-model of Cisplatin-induced emesis, Casopitant inhibits retching and vomiting and reduced nausea-like behaviours 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 possesses a high affinity for brain NK1 receptors in the ferret [2]. |
别名 | GW679769B |
分子量 | 712.72 |
分子式 | C31H39F7N4O5S |
CAS No. | 414910-30-8 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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