Eltrombopag Olamine NEW
| Price | $36 | $58 | $92 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Eltrombopag Olamine | CAS No.: 496775-62-3 |
| Purity: 99.94% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Eltrombopag Olamine |
| Description | Eltrombopag Olamine (Eltrombopag diethanolamine salt) is an orally active small-molecule, nonpeptide thrombopoietin receptor agonist that stimulates megakaryopoiesis. It binds to and activates the transmembrane domain of the platelet thrombopoietin receptor (TPO-R or CD110), promoting the proliferation and differentiation of megakaryocytic cells and enhancing platelet production. |
| Kinase Assay | 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]. |
| In vitro | 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] |
| In vivo | 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] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 82 mg/mL (145.2 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) |
| Keywords | megakaryocyte | Bacterial | Eltrombopag diethanolamine | blood platelet | SB 497115 | N2C-Tpo | Eltrombopag | Thrombopoietin Receptor | chimpanzee | hematopoiesis | inhibit | SB-497115 | Inhibitor | Eltrombopag Olamine | immune thrombocytopenia | BAF3 | CD34 | hepatocellular carcinomab |
| Inhibitors Related | (S)-(+)-Ibuprofen | AEBSF hydrochloride | Heparin sodium salt |
| Related Compound Libraries | Bioactive Compound Library | Drug Repurposing Compound Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
You may like
Recommended supplier
| Product name | Price | Suppliers | Update time | |
|---|---|---|---|---|
| $0.00/1g |
VIP1Y
|
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
|
2024-07-23 | |
| $10.00/1kg |
VIP1Y
|
Hebei Ganmiao New material Technology Co., LTD
|
2024-06-06 | |
| $85.00/1kg |
VIP2Y
|
Zibo Hangyu Biotechnology Development Co., Ltd
|
2023-11-20 | |
| $0.00/1KG |
VIP3Y
|
Wuhan Senwayer Century Chemical Co.,Ltd
|
2022-11-07 | |
| $0.00/1KG |
VIP3Y
|
Henan Aochuang Chemical Co.,Ltd.
|
2022-09-13 | |
| $10.00/1kg |
Hebei Linwo New Material Technology Co., LTD
|
2022-07-05 | ||
| $1.10/1g |
VIP4Y
|
Dideu Industries Group Limited
|
2022-05-20 | |
| $8.00/1g |
Qiuxian Baitai New Material Co., LTD
|
2021-11-26 | ||
| $15.00/1KG |
Zhuozhou Wenxi import and Export Co., Ltd
|
2021-07-10 | ||
| $0.00/1g |
VIP4Y
|
WUHAN FORTUNA CHEMICAL CO., LTD
|
2021-06-23 |
United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
INQUIRY