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)
英語名:
Fosaprepitant dimeglumine
英語别名:
CS-275;Mk-0517;L785298;Unii-D35fm8T64x;MK0517 dimeglumine;MK 0517 dimeglumine;MK-0517 dimeglumine;Foxapyrtam dimeglumine;osaprepitant Dimeglumine;Fosaprepitant dimeglumine
CBNumber:
CB61105364
化学式:
C30H39F7N5O11P
分子量:
809.63
MOL File:
265121-04-8.mol

ホスアプレピタントメグルミン 物理性質

貯蔵温度 :
Sealed in dry,Store in freezer, under -20°C
溶解性:
≥50.24 mg/mL in DMSO; insoluble in EtOH; ≥13.16 mg/mL in H2O with ultrasonic
外見 :
Powder
酸解離定数(Pka):
Fosaprepitant dimeglumine has four functional groups which have pKa values of 3.05 ± 0.03, 4.92 ± 0.02, 9.67 ± 0.01 and 10.59 ± 0.03. The pka value of 3.05 corresponds to the morpholinium group, the pka of 4.92 corresponds to the monophosphonate group, the pka of 9.67 corresponds to the meglumine counter ion, and the pka of 10.59 corresponds to the triazolinone NH group.
安全性情報
  • リスクと安全性に関する声明
  • 危険有害性情報のコード(GHS)
絵表示(GHS) GHS hazard pictograms
注意喚起語 警告
危険有害性情報
コード 危険有害性情報 危険有害性クラス 区分 注意喚起語 シンボル P コード
H315 皮膚刺激 皮膚腐食性/刺激性 2 警告 GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 強い眼刺激 眼に対する重篤な損傷性/眼刺激 性 2A 警告 GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
注意書き
P280 保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。
P302+P352 皮膚に付着した場合:多量の水と石鹸で洗うこと。
P305+P351+P338 眼に入った場合:水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。
P332+P313 皮膚刺激が生じた場合:医師の診断/手当てを受けるこ と。
P337+P313 眼の刺激が続く場合:医師の診断/手当てを受けること。

ホスアプレピタントメグルミン 価格 もっと(2)

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
Sigma-Aldrich Japan SML2228 ≥98% (HPLC)
Fosaprepitant dimeglumine ≥98% (HPLC)
265121-04-8 10MG ¥20200 2024-03-01 購入
Sigma-Aldrich Japan SML2228 ≥98% (HPLC)
Fosaprepitant dimeglumine ≥98% (HPLC)
265121-04-8 50MG ¥81500 2024-03-01 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

Fosaprepitant dimeglumine belongs to the group of antiemetics. The active substance inhibits part of the vomiting centre. It is used for the treatment of postoperative or chemotherapyinduced nausea and vomiting.

化学的特性

Fosaprepitant dimeglumine is a white to off-white amorphous powder. It is freely soluble in water. The pH of a 1.0 g sample of fosaprepitant dimeglumine, dissolved in 25 mL of water, is approximately 8.3. Fosaprepitant, a prodrug of aprepitant, when administered intravenously is rapidly converted to aprepitant.

使用

Fosaprepitant-d4 Dimeglumine is a labeled analogue of Fosaprepitant Dimeglumine (F727305), a selective neurokinin-1 (NK-1) receptor antahonist. Fosaprepitant is an antiemetic drug, a Aprepitant (A729800) prodrug.

定義

ChEBI: Fosaprepitant dimeglumine is 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 substance 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 It has a role as a prodrug, an antiemetic and a neurokinin-1 receptor antagonist. It contains a fosaprepitant(2-).

適応症

Fosaprepitant dimeglumine is a new drug indicated to prevent nausea and vomiting associated with highly emetogenic cisplatin-based and moderately emetogenic cancer chemotherapy in adults.

生物活性

Fosaprepitant dimeglumine acts as a therapeutic agent to treat chemotherapy-induced nausea and vomiting. It also acts as a weak inhibitor of cytochrome P450 3A4 (CYP3A4).
Fosaprepitant dimeglumine is a Substance P/neurokinin-1 (NK1) receptor antagonist. It is a water soluble prodrug of the antiemetic drug aprepitant.
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.

副作用

Most common adverse reactions in adults (≥2%) are: fatigue, diarrhea, neutropenia, asthenia, anemia, peripheral neuropathy, leukopenia, dyspepsia, urinary tract infection, pain in extremity.
Adverse reactions in pediatrics are similar to adults.

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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ホスアプレピタントメグルミン  スペクトルデータ(1HNMR、MS)


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
  • 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)
  • 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 salt
  • Fosaprepitant dimeglumine, >=99%
  • Fosaprepitant dimegluminer
  • Fosaprepitant 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
  • Forxatriptan Meglumine Reference
  • Fosaprepitant dimeglumine(MK-0517)
  • Fosaprepitant dimeglumine(MK0517,Emend, Inemend)
  • [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
  • Fosaprepitant-d4 Dimeglumine
  • CS-275
  • L785298
  • FOSAPREPITANT DIMEGLUMINE 265121-04-8
  • Fosaprepitant dimeglumine USP/EP/BP
  • Fosaprepitant dimeglumine dimeglumine
  • osaprepitant Dimeglumine
  • Fosaprepitant D4 DimeglumineQ: What is Fosaprepitant D4 Dimeglumine Q: What is the CAS Number of Fosaprepitant D4 Dimeglumine Q: What is the storage condition of Fosaprepitant D4 Dimeglumine Q: What are the applications of Fosaprepitant D4 Dimeglumine
  • Fosaprepitant dimeglumineQ: What is Fosaprepitant dimeglumine Q: What is the CAS Number of Fosaprepitant dimeglumine Q: What is the storage condition of Fosaprepitant dimeglumine Q: What are the applications of Fosaprepitant dimeglumine
  • 265121-04-8 Fosaprepitant dimeglumine
  • (3-(((2R,3S)-2-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)morpholino)methyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonic acid bis (2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentaol
  • (2R,3R,4R,5S)-6-(Methylamino)hexane-1,2,3,4,5-pentaol ((3-(((2R,3S)-2-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)morpholino)methyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonate)(2:1)
  • 1- deoxy -1- (methylamino) -D- glucitol [3-[(2r, 3s)-2-[(1r) -1- [3,5-bis (trifluoromethyl) phenyl] ethoxy ]-3-(4- fluorophenyl) -4- morpholinyl]
  • Fosaprepitant Dimeglumine Impurity
  • {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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