엘트롬보팍
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엘트롬보팍 속성
- 녹는점
- 242-244°C
- 끓는 점
- 656.8±65.0 °C(Predicted)
- 밀도
- 1.33
- 저장 조건
- Keep in dark place,Inert atmosphere,Room temperature
- 용해도
- DMSO(최대 55mg/ml) 또는 에탄올(최대 14mg/ml)에 용해됩니다.
- 물리적 상태
- 고체
- 물리적 상태
- 단단한 모양
- 산도 계수 (pKa)
- -1.26±0.40(Predicted)
- 색상
- 오렌지 레드
- 색상
- 오렌지색
- 안정성
- 제공된 대로 구매일로부터 2년 동안 안정적입니다. DMSO 또는 에탄올 용액은 -20°에서 최대 3개월 동안 보관할 수 있습니다.
- 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
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
유해 물질 데이터 | 496775-61-2(Hazardous Substances Data) |
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엘트롬보팍 C화학적 특성, 용도, 생산
개요
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.
화학적 성질
Orange to Red Solid용도
Eltrombopag (SB-497115-GR, Promacta, Revolade) is a small molecule agonist of the c-mpl (TpoR) receptor with an IC50 of 0.69 μM for the inhibition of hERG K+ channel tail current. In preclinical studies, the compound was shown to interact selectively with정의
ChEBI: A hydrazine in which each nitrogen atom is substituted, one by a 3'-carboxy-2-hydroxy[1,1'-biphenyl]-3-yl group and the other by a 1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene group. A small molecule agonist of the c-mpl (TpoR) receptor (the physiological target of the hormone thrombopoietin), it has been developed as a medication for conditions that lead to thrombocytopenia (abnormally low platelet counts).Synthesis
The synthesis of Eltrombopag is as follows:At room temperature, add 8.02g (20.0mmol) compound of formula V, 3.98g (24.0mmol) 3-carboxyphenylboronic acid, 8.48g (80.0mmol) sodium carbonate, 1.46g (2.0mmol) PdCl2dppf into a 250mL three-necked flask, 80mL ethanol, 65mL water, nitrogen protection, heated to 80, reacted for 10h, cooled to room temperature, added 60mL water, filtered, the filtrate was adjusted to pH 1-2 with 2M hydrochloric acid, a red solid was precipitated, filtered, and the filter cake was ethanol/water ( v/v=1:1, 40mL) beating, filtering, and drying to obtain 7.58g, the yield is 85.8%, and the purity is 99.40%.
![synthesis of Eltrombopag.png synthesis of Eltrombopag.png](/NewsImg/2022-12-07/6380602923822135614174581.jpg)
엘트롬보팍 준비 용품 및 원자재
원자재
준비 용품
엘트롬보팍 공급 업체
글로벌( 297)공급 업체
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Zibo Hangyu Biotechnology Development Co., Ltd | +86-0533-2185556 +8617865335152 |
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Nanjing ChemLin Chemical Industry Co., Ltd. | 025-83697070 |
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