Eltrombopag Diolamine
Eltrombopag Olamine
CAS: 496775-62-3
Molecular Formula: C27H29N5O5
Eltrombopag Diolamine - Names and Identifiers
| Name | Eltrombopag Olamine |
| Synonyms | Revolade Promacta SB-497115-GR UNII-4U07F515LG Unii-4U07F515lg Eltrombopag olamine Eltrombopag Olamine EltroMbopag IMpurity Eltrombopag Diolamine EltroMbopag OlaMine API Eltrombopag Olamine [USAN] EltroMbopag diethanolaMine salt |
| CAS | 496775-62-3 |
| EINECS | 629-876-8 |
| InChI | InChI=1/C25H22N4O4.2C2H7NO/c1-14-10-11-19(12-15(14)2)29-24(31)22(16(3)28-29)27-26-21-9-5-8-20(23(21)30)17-6-4-7-18(13-17)25(32)33;2*3-1-2-4/h4-13,26,30H,1-3H3,(H,32,33);2*4H,1-3H2/b27-22-; |
Eltrombopag Diolamine - Physico-chemical Properties
| Molecular Formula | C27H29N5O5 |
| Molar Mass | 503.56 |
| Solubility | 10 mM in DMSO |
| Storage Condition | under inert gas (nitrogen or Argon) at 2–8 °C |
| In vitro study | Half maximal effective concentration of Eltrombopag (EC50) in mouse BAF3 cells transfected with a STAT-activated IRF-1 promoter-controlled luciferase reporter gene and human TpoR (BAF3/IRF-1/hTpoR) is 0.27 μm. Eltrombopag activates the receptor through interaction with metal ions (e. G., Zn2) and specific transmembrane and near-membrane domain TpoR protein amino acids. In N2C-Tpo cells, Eltrombopag (30 μm) caused activation of STAT5 as detected by Western blotting with an anti-phosphorylated STAT5 antibody. In BrdU experiments performed in BAF3/hTpoR cells, Eltrombopag activated cell proliferation after two days of incubation, with an EC50 of 0.03 μm. Eltrombopag also induces hematopoietic stem cells to differentiate into megakaryocyte progenitors. Eltrombopag dose-dependently increased the differentiation of bone marrow CD34 cells into CD41 megakaryocytes with an EC50 of 0.1 μm. Eltrombopag inhibited the proliferation of N2C-Tpo cells and HEL92.1.7 cells, and the IC50 was 20.7 μg/ml and 2.3 mg/mL, respectively. Eltrombopag (20 μg/ml) resulted in a progressive decrease in the rate of cell division, cell cycle arrest in the G1 phase, and increased differentiation of human and murine leukocytes. In HL60 cells, Eltrombopag (5 μg/ml) showed a clear differentiation signal, the nucleus in the tissue was significantly changed, and the ratio of cytoplasm/nucleus increased. Eltrombopag (5 μg/ml) caused an increase in CD11b, which is consistent with the pro-macrophage state in U937 cells, and caused an increase in CD11b in urethan cells. In HL60 cells, Eltrombopag caused a dose-dependent decrease in free ions in leukocytes. |
| In vivo study | Eltrombopag (10 mg/kg/day) increased the number of platelets twofold in one of the three gorillas and 1.5-fold in the other two about one week after administration of Eltrombopag (1 mg/ml) prolonged survival time of leukemia model mice. |
Eltrombopag Diolamine - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.771 ml | 8.855 ml | 17.711 ml |
| 5 mM | 0.354 ml | 1.771 ml | 3.542 ml |
| 10 mM | 0.177 ml | 0.886 ml | 1.771 ml |
| 5 mM | 0.035 ml | 0.177 ml | 0.354 ml |
Last Update：2024-01-02 23:10:35
Eltrombopag Diolamine - Reference Information
| use | eltrombopalethanolamine can be used to treat thrombocytopenia in patients with chronic idiopathic thrombocytopenic purpura (ITP) after splenectomy after glucocorticoid drugs, ineffective immunoglobulin therapy or splenectomy. |
| Biological activity | Eltrombopag Olamine (SB-497115-GR, SB497115) are small molecules, c-mpl (TpoR) receptor agonists, which inhibit hERG K channel tail current, IC50 is 0.69 μM. |
| Target | Value |
Last Update：2024-04-10 22:29:15
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Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
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Product Name: Eltrombopag (Olamine) Visit Supplier Webpage Request for quotationCAS: 496775-62-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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