Eltrombopag(Synonyms: 艾曲波帕; SB-497115)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白、同位素标记物，专注于信号通路和疾病研究领域。
Eltrombopag (Synonyms: 艾曲波帕; SB-497115) 纯度: 99.82%

Eltrombopag (SB-497115) 是一种具有口服活性的 thrombopoietin-receptor 非肽激动剂。Eltrombopag 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 可用于心血管的研究。Eltrombopag 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 还可诱导肝癌细胞凋亡 (apoptosis)。

Eltrombopag(Synonyms: 艾曲波帕; SB-497115)

Eltrombopag Chemical Structure

CAS No. : 496775-61-2

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥858 In-stock
10 mg ￥780 In-stock
50 mg ￥2350 In-stock
100 mg ￥2800 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Eltrombopag 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • Immunology/Inflammation Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Drug Repurposing Compound Library
  • Anti-Cardiovascular Disease Compound Library
  • Antibacterial Compound Library
  • Anti-COVID-19 Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Rare Diseases Drug Library
  • Children’s Drug Library
  • EMA-Approved Drug Library
  • FDA-Approved Anticancer Drug Library

生物活性

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. Eltrombopag can be used for the research of cardiovascular. Eltrombopag also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag can induce apoptosis in 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 inhibits Pneumococcal growth with MIC50 of 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) inhibits Staphylococcus aureus growth with an MIC50 of 1.5 mg/L, and exhibits higher potency when co-treats with Vancomycin (HY-B0671) with an MIC50 of 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Murine BAF3 cells
Concentration: 0.002-50 μM
Incubation Time: 4 h
Result: Effectively inhibited murine BAF3 cells with human TpoR with an EC50 value of 0.27 μM.

[1][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 EC50 of 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 EC50 value 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.

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; i.p.; once a day for 2 days) significantly reduces mean S. aureus counts in mice nasal infection[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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; injected S. aureus (5 × 108 CFU 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 × 106 CFU/lung) in the nasal infection model compared with control PBS (5.2 × 107 CFU/lung) mice.

Clinical Trial

分子量

442.47

Formula

C25H22N4O4
CAS 号

496775-61-2
中文名称

艾曲波帕；伊屈泼帕
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 8.33 mg/mL (18.83 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2600 mL 11.3002 mL 22.6004 mL
5 mM 0.4520 mL 2.2600 mL 4.5201 mL
10 mM 0.2260 mL 1.1300 mL 2.2600 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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 mg/mL (2.26 mM); Clear solution

    此方案可获得 ≥ 1 mg/mL (2.26 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 10.0 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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务