Eltrombopag is an agonist of thrombopoietin-receptor (TpoR) and can stimulate thrombopoiesis.
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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]. |
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NCT01864512 | - | Withdrawn(No eligible patient ...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 << | |
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 |
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 |