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艾曲波帕 /Eltrombopag {[allProObj[0].p_purity_real_show]}

货号:A157281 同义名: SB-497115

Eltrombopag is an agonist of thrombopoietin-receptor (TpoR) and can stimulate thrombopoiesis.

Eltrombopag 化学结构 CAS号:496775-61-2
Eltrombopag 化学结构
CAS号:496775-61-2
Eltrombopag 3D分子结构
CAS号:496775-61-2
Eltrombopag 化学结构 CAS号:496775-61-2
Eltrombopag 3D分子结构 CAS号:496775-61-2
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Eltrombopag 纯度/质量文件 产品仅供科研

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Eltrombopag 生物活性

描述 Eltrombopag (SB-497115) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia and the research of cardiovascular. Eltrombopag also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Otherwise, Eltrombopag can induce apoptosis in hepatocellular carcinomab (HCC) as well[1].[2].[3].[4].[5].
体外研究

Treated with 0.002-50 μM Eltrombopag for 4 h, Eltrombopag effectively inhibits murine BAF3 cells with human TpoR with an EC50 value of 0.27 μM[1].

Eltrombopag (30 μM; 120 min) affects the activities of p-STAT5 in N2C-Tpo cells and in megakaryocytes[1].

Treated with 0.1 nM-10 μM Eltrombopag for 2 days, Eltrombopag promotes BAF3/hTpoR cells proliferation after incubated for 2 days with an EC50 of 0.03 μM[1].

Otherwise, Eltrombopag efficiently inhibits Pneumococcal growth with MIC50 of 0.3 mg/L, but shows no activity against Gram-negative bacteria[3].

In vitro studies reveal that Eltrombopag, at concentrations ranging from 0 to 200 mg/L over a 24-hour period in Caco-2 and HepG2 cells, suppresses the growth of Staphylococcus aureus, achieving a minimum inhibitory concentration (MIC50) of 1.5 mg/L. Its efficacy increases in combination with Vancomycin, lowering the MIC50 to 1.2 mg/L[3].

Eltrombopag, at a dosage of either 0 or 10 μg/mL applied over 72 hours, significantly induces cell cycle arrest at the G0/G1 phase in Huh7 cells[5].

Additionally, Eltrombopag demonstrates anti-proliferative effects against HCC cell lines when administered at concentrations ranging from 0.1 to 100 μg/mL over a 72-hour period[5].

In vitro studies reveal that Eltrombopag, at concentrations ranging from 0 to 200 mg/L over a 24-hour period in Caco-2 and HepG2 cells, suppresses the growth of Staphylococcus aureus, achieving a minimum inhibitory concentration (MIC50) of 1.5 mg/L. Its efficacy increases in combination with Vancomycin, lowering the MIC50 to 1.2 mg/L[3].

Eltrombopag 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00529568 Hepatitis C, Chronic Phase 3 Completed - -
NCT00370331 Purpura, Thrombocytopaenic, Id... 展开 >>iopathic 收起 << Phase 3 Completed - -
NCT01864512 - Withdrawn(No eligible patient ... 展开 >>was enrolled.) 收起 << April 2014 China, Shandong ... 展开 >> Qilu Hospital, Shandong University Jinan, Shandong, China, 250012 收起 <<

Eltrombopag 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.

[3]Lee H, et al. Repurposing Eltrombopag for Multidrug Resistant Staphylococcus aureus Infections. Antibiotics (Basel). 2021 Nov 9;10(11):1372.

[4]Juan Zhu, et al. Identification of Eltrombopag as a Repurposing Drug Against Staphylococcus epidermidis and its Biofilms. Curr Microbiol. 2021 Feb 21.

[5]Kurokawa T, et al. The Eltrombopag antitumor effect on hepatocellular carcinoma. Int J Oncol. 2015 Nov;47(5):1696-702.

Eltrombopag 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.26mL

0.45mL

0.23mL

11.30mL

2.26mL

1.13mL

22.60mL

4.52mL

2.26mL

Eltrombopag 技术信息

CAS号496775-61-2
分子式C25H22N4O4
分子量 442.47
别名 SB-497115
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 7 mg/mL(15.82 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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