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CAS NO.265121-04-8
low price fosaprepitant diMegluMine good supplier in China
One of the most debilitating side effects of cancer treatment is CINV. Although concomitant anti-emetic agents have been prevalent for the past two decades, 50 60% of patients are still plagued by CINV. To meet this need, fosaprepitant dimeglumine has been launched as a water-soluble, phosphoryl pro-drug of aprepitant for intravenous applications. This pro-drug is rapidly converted to aprepitant in vivo, which has a high affinity for the NK-1 receptor (IC50= 90 50 pM for the displacement of [125I]-substance P from hNK-1 expressed in CHO cells); antagonism 606 Shridhar Hegde and Michelle Schmidt of NK-1 prevents binding of the endogenous substance P that is known to induce vomiting. Fosaprepitant is prepared by the regioselective phosphorylation of aprepitant with dibenzylphosphoryl chloride followed by catalytic hydrogenolysis in the presence of N-methyl-Dglucamine. It is approved for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly and moderately emetogenic cancer chemotherapy.
Fosaprepitant dimeglumine is a water-soluble prodrug form of the neurokinin-1 receptor antagonist aprepitant Formulations containing fosaprepitant dimeglumine have been used to prevent chemotherapy-induced nausea and vomiting
Name | Fosaprepitant dimeglumine |
CAS | 265121-04-8 |
MF | C60H78F14N10O20P2 |
MW | 1587.24 |
EINECS | 682-419-4 |
Appearance | White Powder |
Categories | API;Antiemetic;Pharmaceutical |
Uses | Fosaprepitant dimeglumine is approved for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly and moderately emetogenic cancer chemotherapy. |