货号	规格	价格	上海	北京	珠海	重庆	武汉
V46197-1mg	≥98%	￥1800.00 V46197-1mg ￥1800.00 3-5天	0 货期：3-5天	-	-	-	-
V46197-5mg	≥98%	￥3990.00 V46197-5mg ￥3990.00 3-5天	0 货期：3-5天	-	-	-	-
V46197-10mg	≥98%	￥6400.00 V46197-10mg ￥6400.00 3-5天	0 货期：3-5天	-	-	-	-
V46197-25mg	≥98%	￥11500.00 V46197-25mg ￥11500.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

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).

靶点：

NK1R;CYP3A4

体外研究：

In a ferret-model of Cisplatin- induced emesis, Casopitant (GW679769) inhibits retching and vomiting and reduced nausea-like behaviours in a dose-dependent manner. The pharmacokinetics and brain penetration of casopitant are studied in the ferret-model of cisplatin-induced emesis. 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; suggesting that the pharmacologic activity of Casopitant in the ferret is largely attributable to the parent compound. Casopitant possesses a high affinity for brain NK1 receptors in the ferret[2].

保存条件：

2-8°C, 干燥

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.403 ml	7.015 ml	14.031 ml
5 mM	0.281 ml	1.403 ml	2.806 ml
10 mM	0.14 ml	0.702 ml	1.403 ml
50 mM	0.028 ml	0.14 ml	0.281 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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