Eltrombopag Olamine|496775-62-3|(艾曲波帕乙醇胺盐; Eltrombopag diethanolamine salt; SB-497115GR)-陌孚医药/Medlife

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Eltrombopag Olamine (Synonyms: 艾曲波帕乙醇胺盐; Eltrombopag diethanolamine salt; SB-497115GR)

目录号: PL11894 纯度: ≥99%

CAS No. :496775-62-3

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中文名称	Eltrombopag Olamine
中文别名	艾曲波帕乙醇胺;ELTROMBOPAG OL胺;艾曲波帕;艾曲泊帕;艾曲泊帕乙醇胺;伊曲波帕乙醇胺;伊屈波帕;伊屈泼帕乙醇胺;艾曲泊帕杂质13;艾曲波帕乙醇胺盐
英文名称	Eltrombopag Olamine
英文别名	2-aminoethanol,3-[(5E)-5-[[2-(3,4-dimethylphenyl)-5-methyl-3-oxo-1H-pyrazol-4-yl]hydrazinylidene]-6-oxocyclohexa-1,3-dien-1-yl]benzoic acid;EltroMbopag;Eltrombopag Diolamine;Eltrombopag olamine;Revolade;(1,1'-Biphenyl)-3-carboxylic acid, 3'-((2Z)-(1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene)hydrazino)-2'-hydroxy-, compound with 2-aminoethanol (1:2);3'-((2Z)-2-(1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene)diazanyl)-2'-hydroxybiphenyl-3-carboxylic acid compound with 2-aminoethanol (1:2);Eltrombopag diethanolamine salt;Eltrombopag Olamine [USAN];Promacta;Sb 497115gr;SB-497115GR;SB-497115-GR;Unii-4U07F515lg;3'-[(2Z)-2-[1-(3,4-Dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazinyl]-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid compd. with 2-aminoethanol;Eltrombopag olamine;Sb 497115gr;Unii-4U07F515lg;Eltrombopag (Olamine);Eltrombopag Olamine
Cas No.	496775-62-3
分子式	C₂₅H₂₂N₄O₄^.₂(C₂H₇NO)
分子量	564.64
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Eltrombopag Olamine (Eltrombopag diethanolamine salt) 是一种具有口服活性的 thrombopoietin-receptor 非肽激动剂。Eltrombopag Olamine 可促血小板的活性，用于治疗血小板计数低的慢性免疫性血小板减少症。Eltrombopag Olamine 可用于心血管的研究。Eltrombopag Olamine 对多药耐药的金黄色葡萄球菌 (Staphylococcus aureus) 也有很强的抑制作用。Eltrombopag Olamine 还可诱导肝癌细胞凋亡 (apoptosis)。

生物活性

Eltrombopag Olamine (Eltrombopag diethanolamine salt) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag Olamine owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag Olamine can be used for the research of cardiovascular. Eltrombopag Olamine also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag Olamine can induce apoptosis in hepatocellular carcinomab (HCC) as well.

性状

Solid

IC50 & Target[1][2]

Thrombopoietin Receptor, Staphylococcus aureus, Apoptosis

体外研究(In Vitro)

Eltrombopag (0.002-50 μM; 4 h) possesses activity in murine BAF3 cells transfected with the luciferase reporter gene.
Eltrombopag (30 μM; 120 min) affects the activates of p-STAT5 in N2C-Tpo cells.
Eltrombopag (30 μM; 120 min) activates p-STAT5 in megakaryocytes.
Eltrombopag (0.1 nM-10 μM; 30 min) stimulates proliferation of BAF3/hTpoR cells.
Eltrombopag (0.03-3 μM; 10 days) increases the differentiation of bone marrow CD34 cells into CD41 megakaryocytes.
Eltrombopag (0-3 μM; 72 h) affects N2C-Tpo cell apoptosis.
Eltrombopag efficiently inhibits Pneumococcal growth with MIC50 of 0.3 mg/L, but shows no activity against Gram-negative bacteria.
Eltrombopag (0-200 mg/L; 24 h; Caco-2 and HepG2 cells) inhibits Staphylococcus aureus growth with an MIC50 of 1.5 mg/L, and exhibits higher potency when co-treats with

体内研究(In Vivo)

Eltrombopag Olamine (10 mg/kg; p.o. once a day for 5 days) shows good tolerance in chimpanzees.
Eltrombopag Olamine (17.6 mg/kg; IP; once a day for 2 days) significantly reduces mean S. aureus counts in mice nasal infection. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Erickson-Miller CL, et al. Preclinical activity of eltrombopag (SB-497115), an oral, nonpeptide thrombopoietin receptor agonist. Stem Cells. 2009 Feb;27(2):424-30.
[2]. Erickson-Miller CL, et al. Discovery and characterization of a selective, nonpeptidyl thrombopoietin receptor agonist. Exp Hematol. 2005 Jan;33(1):85-93.

溶解度数据	In Vitro: DMSO : ≥ 50 mg/mL (88.55 mM)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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