ホスアプレピタントメグルミン化学構造式

ホスアプレピタントメグルミン

化学名:ホスアプレピタントメグルミン

CAS番号.265121-04-8

英語名:Fosaprepitant dimeglumine

CBNumberCB61105364

MFC30H39F7N5O11P

MW809.63

MOL File265121-04-8.mol

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.
色	White to off-white

危険有害性情報のコード(GHS)

ホスアプレピタントメグルミン価格

製品番号	包装	価格	製品説明	購入
Sigma-Aldrich Japan SML2228	10MG	￥20200	≥98% (HPLC)	購入
Sigma-Aldrich Japan SML2228	50MG	￥81500	≥98% (HPLC)	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

用途
選択的ニューロキニンNK受容体拮抗薬制吐
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生産企業

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

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ホスアプレピタントメグルミン

危険有害性情報のコード(GHS)

ホスアプレピタントメグルミン 価格

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

ホスアプレピタントメグルミン 生産企業

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

ホスアプレピタントメグルミン価格

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

ホスアプレピタントメグルミン生産企業

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