Eltrombopag OlamineC-mpl agonist CAS# 496775-62-3 |
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Quality Control & MSDS
3D structure
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| Cas No. | 496775-62-3 | SDF | Download SDF |
| PubChem ID | 9915926 | Appearance | Powder |
| Formula | C29H36N6O6 | M.Wt | 564.63 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Eltrombopag diethanolamine salt; SB-497115GR | ||
| Solubility | DMSO : ≥ 50 mg/mL (88.55 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 2-aminoethanol;3-[(5E)-5-[[2-(3,4-dimethylphenyl)-5-methyl-3-oxo-1H-pyrazol-4-yl]hydrazinylidene]-6-oxocyclohexa-1,3-dien-1-yl]benzoic acid | ||
| SMILES | CC1=C(C=C(C=C1)N2C(=O)C(=C(N2)C)NN=C3C=CC=C(C3=O)C4=CC(=CC=C4)C(=O)O)C.C(CO)N.C(CO)N | ||
| Standard InChIKey | TYYXAUPVEKKAFG-HTQZHWFGSA-N | ||
| Standard InChI | InChI=1S/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/h4-13,27-28H,1-3H3,(H,32,33);2*4H,1-3H2/b26-21+;; | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Eltrombopag olamine is a new, orally active thrombopoietin-receptor (c-mpl) agonist that stimulates thrombopoiesis.
IC50 Value: 0.27 uM (EC50 in murine BAF3 cells) [1]
Target: thrombopoietin-receptor (c-mpl)
Potential advantages of eltrombopag may include a sustained platelet response and a good tolerability profile.
in vitro: Eltrombopag demonstrated a half maximal effective concentration (EC50) of 0.27 uM 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) [1]. Eltrombopag stimulates the growth of TPO-dependent cell lines via JAK2 and STAT signaling pathways and stimulates isolated human CD34+ cells to become megakaryocytes and produce platelets [2].
in vivo: Twelve weeks of antiviral therapy, with concurrent receipt of eltrombopag or placebo, were completed by 36%, 53%, and 65% of patients receiving 30 mg, 50 mg, and 75 mg of eltrombopag, respectively, and by 6% of patients in the placebo group [3]. Eltrombopag was administered as once-daily oral capsules for 10 days at doses of 5, 10, 25, 30, 50, and 75 mg. The pharmacokinetics of eltrombopag was dose dependent and linear, and eltrombopag increased platelet counts in a dose-dependent manner [4].
Toxicity: There were no apparent differences in the incidence or severity of adverse events in subjects receiving active or placebo study medication [4]. Long-term treatment with eltrombopag was generally safe, well tolerated, and effective in maintaining platelet counts in the desired range [5].
Clinical trial: Eltrombopag In Cord Blood Or Haploidentical Bone Marrow Transplantation. Phase 2 References: | |||||
Eltrombopag Olamine Dilution Calculator
Eltrombopag Olamine Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.7711 mL | 8.8554 mL | 17.7107 mL | 35.4214 mL | 44.2768 mL |
| 5 mM | 0.3542 mL | 1.7711 mL | 3.5421 mL | 7.0843 mL | 8.8554 mL |
| 10 mM | 0.1771 mL | 0.8855 mL | 1.7711 mL | 3.5421 mL | 4.4277 mL |
| 50 mM | 0.0354 mL | 0.1771 mL | 0.3542 mL | 0.7084 mL | 0.8855 mL |
| 100 mM | 0.0177 mL | 0.0886 mL | 0.1771 mL | 0.3542 mL | 0.4428 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Description: IC50 Value: 0.27 uM (EC50 in murine BAF3 cells) [1] Eltrombopag is a new, orally active thrombopoietin-receptor (c-mpl) agonist that stimulates thrombopoiesis. Potential advantages of eltrombopag may include a sustained platelet response and a good tolerability profile. in vitro: Eltrombopag demonstrated a half maximal effective concentration (EC50) of 0.27 uM 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) [1]. Eltrombopag stimulates the growth of TPO-dependent cell lines via JAK2 and STAT signaling pathways and stimulates isolated human CD34+ cells to become megakaryocytes and produce platelets [2]. in vivo: Twelve weeks of antiviral therapy, with concurrent receipt of eltrombopag or placebo, were completed by 36%, 53%, and 65% of patients receiving 30 mg, 50 mg, and 75 mg of eltrombopag, respectively, and by 6% of patients in the placebo group [3]. Eltrombopag was administered as once-daily oral capsules for 10 days at doses of 5, 10, 25, 30, 50, and 75 mg. The pharmacokinetics of eltrombopag was dose dependent and linear, and eltrombopag increased platelet counts in a dose-dependent manner [4]. Toxicity: There were no apparent differences in the incidence or severity of adverse events in subjects receiving active or placebo study medication [4]. Long-term treatment with eltrombopag was generally safe, well tolerated, and effective in maintaining platelet counts in the desired range [5]. Clinical trial: Eltrombopag In Cord Blood Or Haploidentical Bone Marrow Transplantation. Phase 2
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