エルトロムボパグ
- ¥1621800 - ¥1621800
- 化学名: エルトロムボパグ
- 英語名: Eltrombopag
- 別名:エルトロムボパグ;エルトロンボパグ;3'-{2-[(4Z)-1-(3,4-ジメチルフェニル)-3-メチル-5-オキソ-4,5-ジヒドロ-1H-ピラゾール-4-イリデン]ヒドラジン-1-イル}-2'-ヒドロキシ-[1,1'-ビフェニル]-3-カルボン酸;エルトロンボパク;3′-[(Z)-2-[1-(3,4-ジメチルフェニル)-1,5-ジヒドロ-3-メチル-5-オキソ-4H-ピラゾール-4-イリデン]ヒドラジノ]-2′-ヒドロキシビフェニル-3-カルボン酸;SB-497115;3′-[(2Z)-2-[1-(3,4-ジメチルフェニル)-3-メチル-5-オキソ-1H-ピラゾール-4(5H)-イリデン]ヒドラジノ]-2′-ヒドロキシビフェニル-3-カルボン酸
- CAS番号: 496775-61-2
- 分子式: C25H22N4O4
- 分子量: 442.47
- EINECS:610-469-9
- MDL Number:MFCD20926253
1物価
選択条件:
ブランド
- 富士フイルム和光純薬株式会社(wako)
パッケージ
- 1g
- 生産者富士フイルム和光純薬株式会社(wako)
- 製品番号W01MAS090195
- 製品説明
- 英語製品説明(Z)-3'-(2-(1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid
- 包装単位1g
- 価格¥1621800
- 更新しました2018-12-26
- 購入
生産者 | 製品番号 | 製品説明 | 包装単位 | 価格 | 更新時間 | 購入 |
---|---|---|---|---|---|---|
富士フイルム和光純薬株式会社(wako) | W01MAS090195 | (Z)-3'-(2-(1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid |
1g | ¥1621800 | 2018-12-26 | 購入 |
プロパティ
融点 :242-244°C
沸点 :656.8±65.0 °C(Predicted)
比重(密度) :1.33
貯蔵温度 :Keep in dark place,Inert atmosphere,Room temperature
溶解性 :Soluble in DMSO (up to 55 mg/ml) or in ethanol (up to 14 mg/ml).
外見 :solid
酸解離定数(Pka) :-1.26±0.40(Predicted)
色 :Orange
安定性: :Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
InChI :InChI=1S/C25H22N4O4/c1-14-10-11-19(12-15(14)2)29-24(31)22(16(3)28-29)27-26-21-9-5-8-20(23(21)30)17-6-4-7-18(13-17)25(32)33/h4-13,26,30H,1-3H3,(H,32,33)/b27-22-
InChIKey :XDXWLKQMMKQXPV-QYQHSDTDSA-N
SMILES :C1(C2=CC=CC(N/N=C3\C(=O)N(C4=CC=C(C)C(C)=C4)N=C\3C)=C2O)=CC=CC(C(O)=O)=C1
沸点 :656.8±65.0 °C(Predicted)
比重(密度) :1.33
貯蔵温度 :Keep in dark place,Inert atmosphere,Room temperature
溶解性 :Soluble in DMSO (up to 55 mg/ml) or in ethanol (up to 14 mg/ml).
外見 :solid
酸解離定数(Pka) :-1.26±0.40(Predicted)
色 :Orange
安定性: :Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
InChI :InChI=1S/C25H22N4O4/c1-14-10-11-19(12-15(14)2)29-24(31)22(16(3)28-29)27-26-21-9-5-8-20(23(21)30)17-6-4-7-18(13-17)25(32)33/h4-13,26,30H,1-3H3,(H,32,33)/b27-22-
InChIKey :XDXWLKQMMKQXPV-QYQHSDTDSA-N
SMILES :C1(C2=CC=CC(N/N=C3\C(=O)N(C4=CC=C(C)C(C)=C4)N=C\3C)=C2O)=CC=CC(C(O)=O)=C1
安全情報
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注意書き: |
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説明
ITP is an autoimmune disease in which antiplatelet antibodies accelerate the destruction of platelets. In addition, platelet production can be impaired because the antiplatelet antibodies can also damage megakaryocytes. Although the thrombocytopenia of ITP can be severe, signs of bleeding are usually only minor.Eltrombopag is an oral, small-molecule, nonpeptide TPO-receptor agonist. It initiates TPO-receptor signaling by interacting with the transmembrane domain of the receptor, thereby inducing proliferation and differentiation of cells in the megakaryocytic lineage. Eltrombopag is the second TPO-receptor agonist to reach the market behind romiplostim (Nplate), a recombinant fusion protein launched in 2008. Both drugs are specifically indicated for the treatment of thrombocytopenia in patients with chronic ITP who have had an insufficient response to corticosteroids, immunoglobulins, or splenectomy. Eltrombopag is supplied as the ethanolamine salt (also known as eltrombopag olamine).
The most common adverse reactions associated with eltrombopag were nausea, vomiting, mennorrhagia, myalgia, paresthesia and cataracts. Eltrombopag is derived in five synthetic steps starting from 2-bromo-6-nitroanisole, via Suzuki coupling reaction with 3-carboxyphenylboronic acid to a biphenyl intermediate, followed by cleavage of the methyl ether moiety with hydrobromic acid, and reduction of the nitro group to an amino group under catalytic hydrogenation conditions. Subsequently, the amino group is diazotized with sodium nitrite and hydrochloric acid, and the diazonium intermediate is condensed with 1-(3,4-dimethylphenyl)-3-methyl-2,5-dihydro-1H-pyrazol-5-one to produce eltrombopag.
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