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

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

Cat. No.: HY-15306A Purity: 99.96%
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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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 125 In-stock
Solution
10 mM * 1 mL in DMSO USD 125 In-stock
Solid
5 mg USD 73 In-stock
10 mg USD 114 In-stock
50 mg USD 228 In-stock
100 mg USD 294 In-stock
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Eltrombopag Olamine:

Eltrombopag Olamine Related Antibodies

Top Publications Citing Use of Products

    Eltrombopag Olamine 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 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].

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

    Eltrombopag Olamine Related Antibodies

    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].

    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
    Molecular Weight

    564.63

    Formula

    C29H36N6O6
    CAS No.
    Appearance

    Solid

    Color

    Purple to black

    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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" 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
    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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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: ≥ 1.07 mg/mL (1.90 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.07 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.7 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.
    • Protocol 2

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

      Solubility: 1.07 mg/mL (1.90 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.07 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (17.71 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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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, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.96%

    COA (257 KB) HNMR (244 KB) RP-HPLC (311 KB) LCMS (126 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7711 mL 8.8554 mL 17.7107 mL 44.2768 mL
    5 mM 0.3542 mL 1.7711 mL 3.5421 mL 8.8554 mL
    10 mM 0.1771 mL 0.8855 mL 1.7711 mL 4.4277 mL
    15 mM 0.1181 mL 0.5904 mL 1.1807 mL 2.9518 mL
    20 mM 0.0886 mL 0.4428 mL 0.8855 mL 2.2138 mL
    25 mM 0.0708 mL 0.3542 mL 0.7084 mL 1.7711 mL
    30 mM 0.0590 mL 0.2952 mL 0.5904 mL 1.4759 mL
    40 mM 0.0443 mL 0.2214 mL 0.4428 mL 1.1069 mL
    50 mM 0.0354 mL 0.1771 mL 0.3542 mL 0.8855 mL
    60 mM 0.0295 mL 0.1476 mL 0.2952 mL 0.7379 mL
    80 mM 0.0221 mL 0.1107 mL 0.2214 mL 0.5535 mL
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    Eltrombopag Olamine Related Classifications

    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.

    Keywords:

    Eltrombopag496775-62-3Eltrombopag diethanolamine SB-497115GRThrombopoietin ReceptorBacterialApoptosisimmune thrombocytopeniablood platelethematopoiesismegakaryocyteN2C-TpoCD34BAF3chimpanzeehepatocellular carcinomabInhibitorinhibitorinhibit

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