Fosaprepitant dimeglumine(Synonyms: 福沙吡坦二甲葡胺; MK-0517; L785298)

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Fosaprepitant dimeglumine (Synonyms: 福沙吡坦二甲葡胺; MK-0517; L785298) 纯度: 98.05%

Fosaprepitant dimeglumine (MK-0517) 是 Aprepitant (HY-10052) 的前药。Fosaprepitant dimeglumine 是一种神经激肽-1 受体 (neurokinin-1 receptor) 拮抗剂，被开发用于预防化疗引起的恶心呕吐 (CINV)。

Fosaprepitant dimeglumine(Synonyms: 福沙吡坦二甲葡胺; MK-0517; L785298)

Fosaprepitant dimeglumine Chemical Structure

CAS No. : 265121-04-8

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Fosaprepitant dimeglumine 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • Bioactive Compound Library Plus

生物活性

Fosaprepitant dimeglumine (MK-0517) is a prodrug of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV)[1].

IC50 & Target

Neurokinin-1 receptor[1]
体内研究
(In Vivo)

Fosaprepitant dimeglumine (30 mg/kg; i.p.; daily; for 7 days) attenuates tolerance to morphine and increases the antinociceptive effect in in rats[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley rats[1]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection, daily, for 7 days
Result: Increased the antinociceptive effect of morphine compared to control group.

Clinical Trial

分子量

1004.83

Formula

C37H56F7N6O16P
CAS 号

265121-04-8
中文名称

福沙吡坦二甲葡胺
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。
溶解性数据
In Vitro: 

H2O : 50 mg/mL (49.76 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9952 mL 4.9760 mL 9.9519 mL
5 mM 0.1990 mL 0.9952 mL 1.9904 mL
10 mM 0.0995 mL 0.4976 mL 0.9952 mL

*

请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。
参考文献

  • [1]. Pranav Prasoon, et al. Role of fosaprepitant, a neurokinin Type 1 receptor antagonist, in morphine-induced antinociception in rats. Indian J Pharmacol. 2016 Jul-Aug; 48(4): 394-398.

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