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Fosaprepitant dimeglumine salt
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Fosaprepitant dimeglumine salt图片
CAS NO:265121-04-8
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)询价
5mg询价
10mg询价
25mg询价
50mg询价

Fosaprepitant dimeglumine salt (MK-0517) 是 Aprepitant 的前药。
Cas No.265121-04-8
别名福沙吡坦二甲葡胺; MK-0517; L785298
化学名[5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-3-oxo-1H-1,2,4-triazol-2-yl]phosphonic acid;(2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentol
Canonical SMILESCC(C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)OC2C(N(CCO2)CC3=NC(=O)N(N3)P(=O)(O)O)C4=CC=C(C=C4)F.CNCC(C(C(C(CO)O)O)O)O.CNCC(C(C(C(CO)O)O)O)O
分子式C37H56F7N6O16P
分子量1004.83
溶解度≥ 50.2415mg/mL in DMSO
储存条件Store at -20°C,unstable in solution, ready to use.
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Fosaprepitant dimeglumine salt (L-758,298 MK-0517) is an antagonist of neurokinin-1[1].

Fosaprepitant dimeglumine salt has shown the pharmacodynamic function by its active metabolite aprepitant. Fosaprepitanot dimeglumine salt has been found to be a highly selective antagonist of the NK-1 receptor and inhibit the cation of substance P. In addition, Fosaprepitant dimeglumine salt has been exhibited to have the effect on cisplatin induced emesis in the classical ferret model. Besides, because of the brain penetrating of aprepitant, Fosaprepitant dimeglumine salt has been revealed to have a very high affinity for the NK-1 receptor and increase the efficacy by dexamethasone, granisetron and so on. Fosaprepitant dimeglumine salt has been evaluated to use in the prevention of chemotherapy-induced nausea and vomiting (CINV) by combination with a 5-HT3 antagonist and a steroid [1].

References:
[1] Van Belle SJ1, Cocquyt V. Fosaprepitant dimeglumine (MK-0517 or L-785,298), an intravenous neurokinin-1 antagonist for the prevention of chemotherapy induced nausea and vomiting.Expert Opin Pharmacother. 2008 Dec; 9(18):3261-70.

 
 
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