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Eltrombopag

Eltrombopag

产品编号 T2562   CAS 496775-61-2
别名: SB-497115, SB-497115-GR, 艾曲波帕

Eltrombopag (SB-497115-GR) 是一种具有巨核细胞生成刺激活性的口服活性血小板生成素受体激动剂,可结合并刺激血小板血小板生成素受体,用于血小板减少的某些病症研究。

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Eltrombopag Chemical Structure
Eltrombopag, CAS 496775-61-2
规格 价格/CNY 货期 数量
1 mg ¥ 197 现货
5 mg ¥ 393 现货
10 mg ¥ 647 现货
25 mg ¥ 1,160 现货
50 mg ¥ 1,890 现货
100 mg ¥ 2,320 现货
200 mg ¥ 3,460 现货
500 mg ¥ 5,530 现货
1 mL * 10 mM (in DMSO) ¥ 672 现货
其他形式的 Eltrombopag:
产品目录号及名称: Eltrombopag (T2562)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Eltrombopag (SB-497115-GR), an orally active thrombopoietin receptor agonist with megakaryopoiesis stimulating activity, binds to and stimulates the platelet thrombopoietin receptor (TPO-R or CD110).
体外活性 Eltrombopag demonstrates a half maximal effective concentration (EC50) of 0.27 μM in murine BAF3 cells transfected with the luciferase reporter gene under direction of the STAT-activated IRF-1 promoter and human TpoR (BAF3/IRF-1/hTpoR). Eltrombopag activates the receptor by association with metal ions (i.e., Zn2+) and specific amino acids within the transmembrane and juxtamembrane domains of the TpoR. Eltrombopag (30 μM) results in activation of STAT5 in N2C-Tpo cells, as detected with an antiphospho-STAT5 antibody on Western blots. Eltrombopag stimulates proliferation after a 2-day incubation with an EC50 of 0.03 μM in a BrdU assay conducted in BAF3/hTpoR cells. Eltrombopag also induces differentiation of hematopoietic stem cells into committed megakaryocyte progenitor cells. Eltrombopag increases the differentiation of bone marrow CD34+ cells into CD41+ megakaryocytes in a dose-dependent manner with an EC50 of 0.1 μM. [1] Eltrombopag inhibits N2C-Tpo cell and HEL92.1.7 cell proliferating with IC50 of 20.7 μg/mL and 2.3 μg/mL.[2] Eltrombopag (20 μg/mL) leads to a decreased cell division rate, a block in G(1) phase of cell cycle, and increased differentiation in human and murine leukemia cells. Eltrombopag (5 μg/mL) shows clear signs of differentiation, significant changes in the organization of the nuclear contents, and an increase in the cytoplasm/nucleus ratio in HL60 cells. Eltrombopag (5 μg/mL) causes an increase in CD11b, which is consistent with a premacrophage state in U937 cells, and also causes an increase in CD11b in URE cells. Eltrombopag leads to a reduction in free intracellular iron in leukemic cells in a dose-dependent manner in HL60 cells. [3]
体内活性 Eltrombopag (10 mg/kg per day) increases platelet counts over twofold approximately 1 week after the last dose for one chimpanzee and approximately 1.5-fold for the other two chimpanzees. [1] Eltrombopag (1 mg/mL) prolongs survival in mouse models of leukemia. [3]
别名 SB-497115, SB-497115-GR, 艾曲波帕
分子量 442.47
分子式 C25H22N4O4
CAS No. 496775-61-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 25 mg/mL (56.5 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.26 mL 11.3002 mL 22.6004 mL 56.501 mL
5 mM 0.452 mL 2.26 mL 4.5201 mL 11.3002 mL
10 mM 0.226 mL 1.13 mL 2.26 mL 5.6501 mL
20 mM 0.113 mL 0.565 mL 1.13 mL 2.8251 mL
50 mM 0.0452 mL 0.226 mL 0.452 mL 1.13 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Erickson-Miller CL, et al. Stem Cells, 2009, 27(2), 424-430. 2. Erickson-Miller CL, et al. Leuk Res, 2010, 34(9), 1224-1231. 3. Roth M, et al. Blood, 2012, 120(2), 386-394.
Rivaroxaban OM-189 AEBSF hydrochloride Argatroban Ozagrel hydrochloride Bivalirudin Imitrodast Ximelagatran

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌活性化合物库 抗癌药物库 抗癌上市药物库 口服活性化合物库 抗COVID-19化合物库 凝血与抗凝化合物库 抗感染化合物库 人代谢物化合物库 经典已知活性库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Eltrombopag 496775-61-2 Proteases/Proteasome Thrombin hepatocellular carcinomab Apoptosis SB-497115 Inhibitor hematopoiesis chimpanzee inhibit SB497115 immune thrombocytopenia CD34 blood platelet BAF3 Thrombopoietin Receptor SB-497115-GR Bacterial N2C-Tpo megakaryocyte SB 497115 艾曲波帕 inhibitor

 

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