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 activethrombopoietin receptornonpeptide 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 resistantStaphylococcus aureus. Eltrombopag Olamine can induceapoptosisin hepatocellular carcinomab (HCC) as well[1][2][3][4][5]. |
| IC50& Target | Thrombopoietin Receptor,Staphylococcus aureus, Apoptosis[1][3][5] |
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[1].Eltrombopag (30 μM; 120 min) affects the activates of p-STAT5 in N2C-Tpo cells[1].Eltrombopag (30 μM; 120 min) activates p-STAT5 in megakaryocytes[1].Eltrombopag (0.1 nM-10 μM; 30 min) stimulates proliferation of BAF3/hTpoR cells[1].Eltrombopag (0.03-3 μM; 10 days) increases the differentiation of bone marrow CD34+cells into CD41+megakaryocytes[1].Eltrombopag (0-3 μM; 72 h) affects N2C-Tpo cell apoptosis[1].
Eltrombopag efficiently inhibitsPneumococcalgrowth with MIC50of 0.3 mg/L, but shows no activity against Gram-negative bacteria[3].
Eltrombopag (0-200 mg/L; 24 h; Caco-2 and HepG2 cells) inhibitsStaphylococcus aureusgrowth with an MIC50of 1.5 mg/L, and exhibits higher potency when co-treats withVancomycin(HY-B0671) with an MIC50of 1.2 mg/L[3].
Eltrombopag (0 or 10 μg/mL; 72 h) significantly induces G0/G1 phase arrest in Huh7 cells[5].
Eltrombopag (0.1-100 μg/mL; 72 h) exhibits anti-proliferative activity against HCC cell lines[5].
Cell Viability Assay[1] | Cell Line: | Murine BAF3 cells | | Concentration: | 0.002-50 μM | | Incubation Time: | 4 hours | | Result: | Effectively inhibited murine BAF3 cells with human TpoR with an EC50value of 0.27 μM. |
Western Blot Analysis[1] | Cell Line: | N2C-Tpo cells and CD34+ | | Concentration: | 30 μM for N2C-Tpo cells; 0, 1, 3 and 10 μM for CD34+ | | Incubation Time: | 120 min for N2C-Tpo cells; 30 min for CD34+ | | Result: | Activated phospho-STAT5 and maximum signal intensity exhibited at 60 minutes after treatment in N2C-Tpo cells.
Dose-dependently activated STAT5 phosphorylation at 30 minutes after treatment in CD34+. |
Cell Proliferation Assay[1] | Cell Line: | BAF3/hTpoR cells | | Concentration: | 0.1 nM-10 μM | | Incubation Time: | 2 days | | Result: | Promoted BAF3/hTpoR cells proliferation after incubated for 2 days with an EC50of 0.03 μM. |
Cell Differentiation Assay[1] | Cell Line: | CD34+ | | Concentration: | 0.003, 0.01, 0.03, 0.1, 0.3, 1 and 3 μM | | Incubation Time: | 10 days | | Result: | Dose-dependently stimulated the differentiation from bone marrow CD34+cells to CD41+megakaryocytes with an EC50value of 0.1 μM. |
Apoptosis Analysis[1] | Cell Line: | N2C-Tpo cells | | Concentration: | 0, 0.003, 0.01, 0.03, 0.1, 0.3, 1 and 3 μM | | Incubation Time: | 72 hours | | Result: | Exhibited dose-dependently antiapoptotic effects N2C-Tpo cells with a concentration over 0.03 μM. |
Cell Proliferation Assay[5] | Cell Line: | Huh7, HepG2 and Hep3B cells (preloaded with iron (500 μg/ml FAC) for 24 h) | | Concentration: | 0.1-100 μg/mL | | Incubation Time: | 72 h | | Result: | Exhibited anti-proliferative activity against HCC cell lines with IC50s of 5.7 μg/ml for Huh7, 5.4 μg/ml for HepG2, and 4.7 μg/ml for Hep3B. |
Cell Cycle Analysis[5] | Cell Line: | Huh7 cells | | Concentration: | 0 or 10 μg/mL | | Incubation Time: | 72 h | | Result: | Significantly induced G0/G1 phase arrest. |
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体内研究
(In Vivo) | Eltrombopag Olamine (10 mg/kg; p.o. once a day for 5 days) shows good tolerance in chimpanzees[1].
Eltrombopag Olamine (17.6 mg/kg; IP; once a day for 2 days) significantly reduces meanS. aureuscounts in mice nasal infection[3].
| Animal Model: | Female chimpanzees[1] | | Dosage: | 10 mg/kg | | Administration: | Oral gavage; 10 mg/kg once a day; for 5 days | | Result: | Appeared a goes up and then goes back tendency of platelet counts after treatment, and showed no bad effects of hematology, coagulation, or clinical chemistry parameters on animal. |
| Animal Model: | C57BL/6 male mice (7 weeks, 20-22 g; injectedS. aureus(5 × 108CFU suspended in 40 μL PBS) into the nasal cavities)[3] | | Dosage: | 17.6 mg/kg | | Administration: | IP; once a day for 2 days | | Result: | Significantly reduced mean bacterial counts (5.0 × 106CFU/lung) in the nasal infection model compared with control PBS (5.2 × 107CFU/lung) mice. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : ≥ 50 mg/mL(88.55 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 1.7711 mL | 8.8554 mL | 17.7107 mL | | 5 mM | 0.3542 mL | 1.7711 mL | 3.5421 mL | | 10 mM | 0.1771 mL | 0.8855 mL | 1.7711 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 1.07 mg/mL (1.90 mM); Clear solution
此方案可获得 ≥ 1.07 mg/mL (1.90 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 10.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 1.07 mg/mL (1.90 mM); Suspended solution; Need ultrasonic
此方案可获得 1.07 mg/mL (1.90 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 10.7 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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