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Purity: ≥98%
Eltrombopag Olamine (SB-497115-GR, SB497115; trade names: Promacta; Revolade), the olamine salt of Eltrombopag which is a member of the biarylhydrazone compounds, is a nonpeptide agonist of the thrombopoietin receptor (TpoR) approved as a medication to treat thrombocytopenia and severe aplastic anemia.
| ln Vitro |
When luciferase reporter gene is transfected into murine BAF3 cells, eltrombopag (0.002-50 μM; 4 h) exhibits activity[1]. In N2C-Tpo cells, eltrombopag (30 μM; 120 min) had an impact on p-STAT5 activation[1]. In megakaryocytes, eltrombopag (30 μM; 120 min) stimulates p-STAT5[1]. The proliferation of BAF3/hTpoR cells is stimulated by eltrombopag (0.1 nM-10 μM; 30 min)[1]. Bone marrow CD34+ cells are more likely to differentiate into CD41+ megakaryocytes when treated with elotrombopag (0.03-3 μM) for ten days[1]. N2C-Tpo cell apoptosis is impacted by eltrombopag (0-3 μM; 72 h)[1]. With a MIC50 of 0.3 mg/L, eloxacoum effectively suppresses the growth of pneumococcal bacteria, while it has no effect on Gram-negative bacteria[3]. With a MIC50 of 1.5 mg/L, eltrombopag (0-200 mg/L; 24 h) suppresses the development of Staphylococcus aureus. When combined with vancomycin, which has a MIC50 of 1.2 mg/L, eltrombopag's potency is increased[3]. Eltrombopag strongly promotes G0/G1 phase arrest in Huh7 cells (0 or 10 μg/mL; 72 h)[5]. Eltrombopag has anti-proliferative effect against HCC cell lines at concentrations of 0.1-100 μg/mL for 72 hours[5].
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| ln Vivo |
In chimpanzees, eltrombopag Olamine (10 mg/kg; po once daily for five days) exhibits good tolerance[1]. Mean S is greatly decreased by elotrombopag Olamine (17.6 mg/kg; IP; once daily for two days). Mouse nasal infections with numbers of aureus[3].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Murine BAF3 cells Tested Concentrations: 0.002-50 μM Incubation Duration: 4 hrs (hours) Experimental Results: Effectively inhibited murine BAF3 cells with human TpoR with an EC50 value of 0.27 μM. Western Blot Analysis[1] Cell Types: N2C-Tpo cells and CD34+ Tested Concentrations: 30 μM for N2C-Tpo cells; 0, 1, 3 and 10 μM for CD34+ Incubation Duration: 120 min for N2C- Tpo cells; 30 min for CD34+ Experimental Results: Activated phospho-STAT5 and maximum signal intensity demonstrated at 60 minutes after treatment in N2C-Tpo cells. Dose-dependently activated STAT5 phosphorylation at 30 minutes after treatment in CD34+. Cell Proliferation Assay[1] Cell Types: BAF3/hTpoR cells Tested Concentrations: 0.1 nM-10 μM Incubation Duration: 2 days Experimental Results: Promoted BAF3/hTpoR cells proliferation after incubated for 2 days with an EC50 of 0.03 μM. Cell Differentiation Assay[1] Cell Types: CD34+ Tested Concentrations: 0.003, 0.01, 0.03, 0.1, 0.3, 1 and 3 μM Incubation Duration: 10 days Experimental Results: Dose-dependently stimulated the differentiation from bone m |
| Animal Protocol |
Animal/Disease Models: Female chimpanzees[1]
Doses: 10 mg/kg Route of Administration: po (oral gavage); 10 mg/kg one time/day; for 5 days Experimental Results: Appeared a goes up and then goes back tendency of platelet counts after treatment, and demonstrated no bad effects of hematology, coagulation, or clinical chemistry parameters on animal. Animal/Disease Models: C57BL/6 male mice (7 weeks, 20-22 g; injected S. aureus (5 × 108 CFU suspended in 40 µL PBS) into the nasal cavities)[3] Doses: 17.6 mg/kg Route of Administration: IP; one time/day for 2 days Experimental Results: Dramatically decreased mean bacterial counts (5.0 × 106 CFU/lung) in the nasal infection model compared with control PBS (5.2 × 107 CFU/lung) mice. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Minimal information is available on the use of eltrombopag during breastfeeding. One breastfed infant with thrombocytosis at birth that was possibly prolonged by eltrombopag in milk. Until more data become available, romiplostim should be used with careful infant monitoring of infant blood parameters during breastfeeding, especially while nursing a newborn or preterm infant. The manufacturer recommends avoiding breastfeeding during the use of eltrombopag. Based on the drug’s half-life, the drug should be eliminated by the mother 8 days after the last dose. ◉ Effects in Breastfed Infants An infant was born to a mother taking eltrombopag in a maximum dose of 100 mg during pregnancy. At birth, the infant had thrombocytosis, which persisted for a few weeks while the mother was breastfeeding. The extent of breastfeeding and the maternal dose were not stated. The authors felt that the persistence of thrombocytosis in the infant was possibly caused by eltrombopag in milk. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References |
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| Additional Infomation |
See also: Eltrombopag Olamine (annotation moved to).
Drug Indication Revolade is indicated for the treatment of adult patients with primary immune thrombocytopenia (ITP) who are refractory to other treatments (e. g. corticosteroids, immunoglobulins) (see sections 4. 2 and 5. 1). Revolade is indicated for the treatment of paediatric patients aged 1 year and above with primary immune thrombocytopenia (ITP) lasting 6 months or longer from diagnosis and who are refractory to other treatments (e. g. corticosteroids, immunoglobulins) (see sections 4. 2 and 5. 1). Revolade is indicated in adult patients with chronic hepatitis C virus (HCV) infection for the treatment of thrombocytopenia, where the degree of thrombocytopenia is the main factor preventing the initiation or limiting the ability to maintain optimal interferon-based therapy (see sections 4. 4 and 5. 1). Revolade is indicated in adult patients with acquired severe aplastic anaemia (SAA) who were either refractory to prior immunosuppressive therapy or heavily pretreated and are unsuitable for haematopoietic stem cell transplantation (see section 5. 1). |
| Molecular Formula |
C29H36N6O6
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| Molecular Weight |
564.63
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| Exact Mass |
564.269
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| CAS # |
496775-62-3
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| Related CAS # |
Eltrombopag;496775-61-2;(E/Z)-Eltrombopag-13C4;1217230-31-3
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| PubChem CID |
135449331
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| Appearance |
Purple to black solid powder
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| LogP |
3.127
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
41
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| Complexity |
822
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PLILLUUXAVKBPY-SBIAVEDLSA-N
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| InChi Code |
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/h4-13,26,30H,1-3H3,(H,32,33);2*4H,1-3H2/b27-22-
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| Chemical Name |
(Z)-3-(2-(1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene)hydrazinyl)-2-hydroxy-[1,1-biphenyl]-3-carboxyiic acid;2-aminoethan-1-ol (1:2)
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| Synonyms |
SB-497115-GR, SB497115GR; SB497115; SB-497115; SB 497115; trade name: PROMACTA
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.07 mg/mL (1.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.7 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.07 mg/mL (1.90 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 10 mg/mL (17.71 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7711 mL | 8.8554 mL | 17.7107 mL | |
| 5 mM | 0.3542 mL | 1.7711 mL | 3.5421 mL | |
| 10 mM | 0.1771 mL | 0.8855 mL | 1.7711 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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