Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Eltrombopag Olamine (Eltrombopag diethanolamine salt) 是 Eltrombopag 的口服活性乙醇胺盐,是一种血小板生成素(TPO)受体激动剂,用于血小板减少的某些病症研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 253 | 现货 | ||
5 mg | ¥ 393 | 现货 | ||
10 mg | ¥ 647 | 现货 | ||
25 mg | ¥ 1,160 | 现货 | ||
50 mg | ¥ 1,950 | 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) | ¥ 593 | 现货 |
产品描述 | Eltrombopag Olamine (Eltrombopag diethanolamine salt) is the orally active ethanolamine salt of eltrombopag, a small-molecule, nonpeptide thrombopoietin receptor agonist with megakaryopoiesis-stimulating activity. Eltrombopag binds to and stimulates the transmembrane domain of the platelet thrombopoietin receptor (TPO-R or CD110), a member of the hematopoietin receptor superfamily. Activation of TPO-R leads to the proliferation and differentiation of cells in the megakaryocytic lineage and an increase in platelet production. |
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] |
激酶实验 | The high-performance liquid chromatography (HPLC) analyses are carried out using a Fast Acid Column (100×7.8 mm) and a HPX-87H Ion Exclusion Column (300 mm×7.8 mm) in series with 2.5 mM H2SO4 in water as the mobile phase at a flow rate of 0.3 mL/min, at 55°C. This method enabled quantification of D-glucose, ethanol, glycerol, D-xylulose, Ribitol, and xylitol. D-ribose, D-ribulose, and D-arabitol coeluted on the Aminex HPX-87H column. The CarboPac MA-1 column of Dionex ICS-3000 is used to analyze representative culture supernatant samples for the presence of arabitol and xylitol. Samples are run at column temperature of 30°C with 480 mM NaOH at flow rate 0.4 mL/min. The CarboPac MA-1 column separated D-arabitol from D-ribose and D-ribulose, but the alkaline conditions degraded D-ribulose interfering with the quantification of D-ribose.Yeast cells are disrupted with glass beads in 100 mM sodium phosphate buffer pH 7.0 containing phenylmethylsulfonyl fluoride and pepstatin A in final concentrations of 0.17 mg/mL and 0.01 mg/mL, respectively.The activity of NAD+-dependent Gdh2p is measured in a reaction buffer of 0.5 M triethanol amine pH 7.7 and 2 mM NADH. After addition of the cell lysate, the reaction is started by adding a mixture of α-ketoglutarate (100 mM) and NH4Cl (200 mM) to a final concentration of 2.4 mM and 4.9 mM, respectively. The GapB activity is measured. Shortly, the reaction mixture is 500 mM triethanol amine pH 7.8, 1 mM ATP, 2 mM MgCl2, 200 μM NADPH, and 10 μg/mL of phosphoglycerate kinase. 3-phosphoglycerate is added to a final concentration of 5 mM to start the reaction. Activity measurements are performed with a Cobas Mira Plus automated analyzer[2]. |
别名 | Promacta Olamine, Revolade, 艾曲泊帕乙醇胺盐, Eltrombopag diethanolamine salt, SB497115, 艾曲波帕乙醇胺盐, SB-497115GR |
分子量 | 564.63 |
分子式 | C29H36N6O6 |
CAS No. | 496775-62-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 82 mg/mL (145.2 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7711 mL | 8.8554 mL | 17.7107 mL | 44.2768 mL |
5 mM | 0.3542 mL | 1.7711 mL | 3.5421 mL | 8.8554 mL | |
10 mM | 0.1771 mL | 0.8855 mL | 1.7711 mL | 4.4277 mL | |
20 mM | 0.0886 mL | 0.4428 mL | 0.8855 mL | 2.2138 mL | |
50 mM | 0.0354 mL | 0.1771 mL | 0.3542 mL | 0.8855 mL | |
100 mM | 0.0177 mL | 0.0886 mL | 0.1771 mL | 0.4428 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
Eltrombopag Olamine 496775-62-3 Proteases/Proteasome Thrombin megakaryocyte Bacterial Eltrombopag diethanolamine blood platelet SB 497115 N2C-Tpo Eltrombopag Thrombopoietin Receptor chimpanzee hematopoiesis Promacta Olamine inhibit SB-497115 Inhibitor immune thrombocytopenia BAF3 Revolade CD34 艾曲泊帕乙醇胺盐 Eltrombopag diethanolamine salt SB497115 艾曲波帕乙醇胺盐 SB-497115GR hepatocellular carcinomab inhibitor