标签归档：fosaprepitant

Fosaprepitant-d4 dimeglumine(Synonyms: MK-0517-d4; L785298-d4)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Fosaprepitant-d4 dimeglumine (Synonyms: MK-0517-d4; L785298-d4)

Fosaprepitant-d4 (dimeglumine) 是 Fosaprepitant (dimeglumine) 氘代物。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-d4 dimeglumine(Synonyms: MK-0517-d4; L785298-d4)

Fosaprepitant-d4 dimeglumine Chemical Structure

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生物活性

Fosaprepitant-d4 (dimeglumine) is deuterium labeled Fosaprepitant (dimeglumine). 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].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

1008.86

Formula

C37H52D4F7N6O16P
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

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

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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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10 mg ￥750 In-stock
50 mg ￥2700 In-stock
100 mg ￥4500 In-stock
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500 mg   询价  

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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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务