1. Immunology/Inflammation
    Anti-infection
    Apoptosis
  2. Thrombopoietin Receptor
    Bacterial
    Apoptosis
  3. Eltrombopag Olamine

Eltrombopag Olamine  (Synonyms: Eltrombopag diethanolamine salt; SB-497115GR)

Cat. No.: HY-15306A Purity: 99.96%
COA Handling Instructions

Eltrombopag Olamine (Eltrombopag diethanolamine salt) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag Olamine owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag Olamine can be used for the research of cardiovascular. Eltrombopag Olamine also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag Olamine can induce apoptosis in hepatocellular carcinomab (HCC) as well.

For research use only. We do not sell to patients.

Eltrombopag Olamine Chemical Structure

Eltrombopag Olamine Chemical Structure

CAS No. : 496775-62-3

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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Eltrombopag Olamine:

Top Publications Citing Use of Products

    Eltrombopag Olamine purchased from MCE. Usage Cited in: Blood Adv. 2017 Feb 28;1(7):468-476.  [Abstract]

    STAT5 phosphorylation in UT-7/TPO cells stimulated for 15 to 360 minutes with rhTPO (100 ng/mL), TA-316 (100 ng/mL), Eltrombopag (1000 ng/mL), or DMSO (vehicle) are evaluated using BD Phosflow (STAT5, pY694).
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Eltrombopag Olamine (Eltrombopag diethanolamine salt) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag Olamine owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag Olamine can be used for the research of cardiovascular. Eltrombopag Olamine also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag Olamine can induce apoptosis in hepatocellular carcinomab (HCC) as well[1][2][3][4][5].

    IC50 & Target

    Thrombopoietin Receptor, Staphylococcus aureus, Apoptosis[1][3][5]

    In Vitro

    Eltrombopag (0.002-50 μM; 4 h) possesses activity in murine BAF3 cells transfected with the luciferase reporter gene[1].
    Eltrombopag (30 μM; 120 min) affects the activates of p-STAT5 in N2C-Tpo cells[1].
    Eltrombopag (30 μM; 120 min) activates p-STAT5 in megakaryocytes[1].
    Eltrombopag (0.1 nM-10 μM; 30 min) stimulates proliferation of BAF3/hTpoR cells[1].
    Eltrombopag (0.03-3 μM; 10 days) increases the differentiation of bone marrow CD34+ cells into CD41+ megakaryocytes[1].
    Eltrombopag (0-3 μM; 72 h) affects N2C-Tpo cell apoptosis[1].
    Eltrombopag efficiently inhibits Pneumococcal growth with MIC50 of 0.3 mg/L, but shows no activity against Gram-negative bacteria[3].
    Eltrombopag (0-200 mg/L; 24 h; Caco-2 and HepG2 cells) inhibits Staphylococcus aureus growth with an MIC50 of 1.5 mg/L, and exhibits higher potency when co-treats with Vancomycin (HY-B0671) with an MIC50 of 1.2 mg/L[3].
    Eltrombopag (0 or 10 μg/mL; 72 h) significantly induces G0/G1 phase arrest in Huh7 cells[5].
    Eltrombopag (0.1-100 μg/mL; 72 h) exhibits anti-proliferative activity against HCC cell lines[5].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Viability Assay[1]

    Cell Line: Murine BAF3 cells
    Concentration: 0.002-50 μM
    Incubation Time: 4 hours
    Result: Effectively inhibited murine BAF3 cells with human TpoR with an EC50 value of 0.27 μM.

    Western Blot Analysis[1]

    Cell Line: N2C-Tpo cells and CD34+
    Concentration: 30 μM for N2C-Tpo cells; 0, 1, 3 and 10 μM for CD34+
    Incubation Time: 120 min for N2C-Tpo cells; 30 min for CD34+
    Result: Activated phospho-STAT5 and maximum signal intensity exhibited 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 Line: BAF3/hTpoR cells
    Concentration: 0.1 nM-10 μM
    Incubation Time: 2 days
    Result: Promoted BAF3/hTpoR cells proliferation after incubated for 2 days with an EC50 of 0.03 μM.

    Cell Differentiation Assay[1]

    Cell Line: CD34+
    Concentration: 0.003, 0.01, 0.03, 0.1, 0.3, 1 and 3 μM
    Incubation Time: 10 days
    Result: Dose-dependently stimulated the differentiation from bone marrow CD34+ cells to CD41+ megakaryocytes with an EC50 value of 0.1 μM.

    Apoptosis Analysis[1]

    Cell Line: N2C-Tpo cells
    Concentration: 0, 0.003, 0.01, 0.03, 0.1, 0.3, 1 and 3 μM
    Incubation Time: 72 hours
    Result: Exhibited dose-dependently antiapoptotic effects N2C-Tpo cells with a concentration over 0.03 μM.

    Cell Proliferation Assay[5]

    Cell Line: Huh7, HepG2 and Hep3B cells (preloaded with iron (500 μg/ml FAC) for 24 h)
    Concentration: 0.1-100 μg/mL
    Incubation Time: 72 h
    Result: Exhibited anti-proliferative activity against HCC cell lines with IC50s of 5.7 μg/ml for Huh7, 5.4 μg/ml for HepG2, and 4.7 μg/ml for Hep3B.

    Cell Cycle Analysis[5]

    Cell Line: Huh7 cells
    Concentration: 0 or 10 μg/mL
    Incubation Time: 72 h
    Result: Significantly induced G0/G1 phase arrest.
    In Vivo

    Eltrombopag Olamine (10 mg/kg; p.o. once a day for 5 days) shows good tolerance in chimpanzees[1].
    Eltrombopag Olamine (17.6 mg/kg; IP; once a day for 2 days) significantly reduces mean S. aureus counts in mice nasal infection[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Female chimpanzees[1]
    Dosage: 10 mg/kg
    Administration: Oral gavage; 10 mg/kg once a day; for 5 days
    Result: Appeared a goes up and then goes back tendency of platelet counts after treatment, and showed no bad effects of hematology, coagulation, or clinical chemistry parameters on animal.
    Animal Model: 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]
    Dosage: 17.6 mg/kg
    Administration: IP; once a day for 2 days
    Result: Significantly reduced mean bacterial counts (5.0 × 106 CFU/lung) in the nasal infection model compared with control PBS (5.2 × 107 CFU/lung) mice.
    Clinical Trial
    Molecular Weight

    564.63

    Formula

    C29H36N6O6

    CAS No.
    SMILES

    O=C(C1=CC(C2=CC=CC(N/N=C3C(C)=NN(C4=CC=C(C)C(C)=C4)C/3=O)=C2O)=CC=C1)O.NCCO.NCCO

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (88.55 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (3.68 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (3.68 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.96%

    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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