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

Eltrombopag (SB-497115) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag can be used for the research of cardiovascular. Eltrombopag also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag can induce apoptosis in hepatocellular carcinomab (HCC) as well.

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

Eltrombopag Chemical Structure

Eltrombopag Chemical Structure

CAS No. : 496775-61-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 100 In-stock
Solution
10 mM * 1 mL in DMSO USD 105 In-stock
Solid
5 mg USD 61 In-stock
10 mg USD 95 In-stock
50 mg USD 190 In-stock
100 mg USD 245 In-stock
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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of Eltrombopag:

Eltrombopag Related Antibodies

Top Publications Citing Use of Products

    Eltrombopag purchased from MedChemExpress. 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 (SB-497115) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag can be used for the research of cardiovascular. Eltrombopag also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag 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.html" class="link-product" target="_blank">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].

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

    Eltrombopag Related Antibodies

    Cell Viability Assay[1]

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

    [1][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; i.p.; once a day for 2 days) significantly reduces mean S. aureus counts in mice nasal infection[3].

    MedChemExpress (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
    NCT NumberSponsorConditionStart DatePhase
    NCT01286038H. Lee Moffitt Cancer Center and Research Institute|GlaxoSmithKline
    Myelodysplastic Syndrome (MDS)|Thrombocytopenia
    		April 6, 2011Phase 1
    NCT00828750GlaxoSmithKline
    Idiopathic Thrombocytopenic Purpura|Purpura, Thrombocytopenic, Idiopathic
    		May 2008Phase 3
    NCT00833378GlaxoSmithKline
    Hepatitis C
    		January 19, 2009Phase 1
    Molecular Weight

    442.47

    Formula

    C25H22N4O4
    CAS No.
    Appearance

    Solid

    Color

    Yellow to orange

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 8.33 mg/mL (18.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2600 mL 11.3002 mL 22.6004 mL
    5 mM 0.4520 mL 2.2600 mL 4.5201 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 1 mg/mL (2.26 mM); Clear solution

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.94%

    Data Sheet (286 KB) SDS (393 KB)

    COA (252 KB)LCMS (94 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2600 mL 11.3002 mL 22.6004 mL 56.5010 mL
    5 mM 0.4520 mL 2.2600 mL 4.5201 mL 11.3002 mL
    10 mM 0.2260 mL 1.1300 mL 2.2600 mL 5.6501 mL
    15 mM 0.1507 mL 0.7533 mL 1.5067 mL 3.7667 mL
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    Eltrombopag Related Classifications

    Keywords:

    Eltrombopag496775-61-2SB-497115SB497115SB 497115Thrombopoietin ReceptorBacterialApoptosisimmune thrombocytopeniablood platelethematopoiesismegakaryocyteN2C-TpoCD34BAF3chimpanzeehepatocellular carcinomabInhibitorinhibitorinhibit

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