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ホスアプレピタントメグルミン

ホスアプレピタントメグルミン 化学構造式
265121-04-8
CAS番号.
265121-04-8
化学名:
ホスアプレピタントメグルミン
别名:
{3-[((2R,3S)-2-{(1R)-1-[3,5-ビス(トリフル オロメチル)フェニル]エトキシ}-3-(4-フルオロフェニル)モルホリ ン-4-イル)メチル]-5-オキソ-4,5-ジヒドロ-1H-1,2,4 -トリアゾール-1-イル}ホスホン酸=ビス[1-デオキシ-1-(メチル アミノ)-D-グルシトール]塩;ホスアプレピタントメグルミン;フォサプレピタントジメグルミン;ホスアプレピタントメグルミン (JAN)
英語化学名:
Fosaprepitant dimeglumine
英語别名:
Mk-0517;Unii-D35fm8T64x;Fosaprepitant dimeglumine;Fosaprepitant dimegluminer;Fosaprepitant-d4 Dimeglumine;Fosaprepitant diMegluMine salt;Fosaprepitant dimeglumine, >=99%;Fosaprepitant dimeglumine(MK-0517);Fosaprepitant dimeglumine(MK0517,Emend, Inemend);1-DEOXY-1-(METHYLAMINO)-D-GLUCITOL [[(2R,3S]-2-[(1R)-1-[3,5-BIS (TRIFLUOROMETHYL)PHENYL] PHENYL]ETHOXY]-(4-FLUOROPHENYL)
CBNumber:
CB61105364
化学式:
C60H78F14N10O20P2
分子量:
1587.2414868
MOL File:
265121-04-8.mol

ホスアプレピタントメグルミン 物理性質

安全性情報

ホスアプレピタントメグルミン 価格

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入

ホスアプレピタントメグルミン 化学特性,用途語,生産方法

効能

制吐薬, NK1受容体拮抗薬

商品名

プロイメンド (小野薬品工業)

説明

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.

Originator

Merck (United States)

使用

Fosaprepitant is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist

定義

ChEBI: An organoammonium salt obtained by reaction of fosaprepitant with two equivalents of 1-deoxy-1-(methylamino)-D-glucitol. A substance P/neurokinin 1 (NK1) receptor antagonist. Aprepitant is a selective high-affinity antagonist of human subs ance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting and postoperative nausea and vomiting

brand name

IvEmend

ホスアプレピタントメグルミン 上流と下流の製品情報

原材料

準備製品


ホスアプレピタントメグルミン 生産企業

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265121-04-8(ホスアプレピタントメグルミン)キーワード:


  • 265121-04-8
  • Fosaprepitant-d4 Dimeglumine
  • D-Glucitol, 1-deoxy-1-(methylamino)-, (3-(((2R,3S)-2-((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)-4- morpholinyl)methyl)-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl)phosphonate (2:1) (salt)
  • Mk-0517
  • Fosaprepitant dimeglumine(MK-0517)
  • Fosaprepitant dimeglumine(MK0517,Emend, Inemend)
  • Phosphonic acid, (3-(((2R,3S)-2-((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)-4-morpholinyl)methyl)-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl)-, compd. with 1-deoxy-1-(methylamino)-D-glucitol (1:2)
  • Unii-D35fm8T64x
  • [3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoroMethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-Morpholinyl]Methyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl]phosphonate 1-Deoxy-1-(MethylaMino)-D-glucitol
  • 1-Deoxy-1-(MethylaMino)-D-glucitol [3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoroMethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-Morpholinyl]Methyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl]phosphonate
  • 1-DEOXY-1-(METHYLAMINO)-D-GLUCITOL [[(2R,3S]-2-[(1R)-1-[3,5-BIS (TRIFLUOROMETHYL)PHENYL] PHENYL]ETHOXY]-(4-FLUOROPHENYL)
  • Fosaprepitant diMegluMine salt
  • 3-[2(R)-[1(R)-[3,5-Bis(trifluoroMethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)Morpholin-4-ylMethyl]-5-oxo-4,5-dihydro-1H-1,2,4-triazole-1-phosphinic acid bis(N-Methyl-D-glucaMine) salt
  • Fosaprepitant dimeglumine, >=99%
  • Fosaprepitant dimegluminer
  • Fosaprepitant dimeglumine
  • {3-[((2R,3S)-2-{(1R)-1-[3,5-ビス(トリフル オロメチル)フェニル]エトキシ}-3-(4-フルオロフェニル)モルホリ ン-4-イル)メチル]-5-オキソ-4,5-ジヒドロ-1H-1,2,4 -トリアゾール-1-イル}ホスホン酸=ビス[1-デオキシ-1-(メチル アミノ)-D-グルシトール]塩
  • ホスアプレピタントメグルミン
  • フォサプレピタントジメグルミン
  • ホスアプレピタントメグルミン (JAN)
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