[CAS NO. 496775-62-3]  EltrombopagOlamine

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PRODUCTS SPECIFICATIONS [496775-62-3]

Catalog
HY-15306A
Brand
MCE
CAS
496775-62-3

DESCRIPTION [496775-62-3]

Overview

MDLMFCD22380664
Molecular Weight564.63
Molecular FormulaC29H36N6O6
SMILESO=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

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


Summary

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 MIC 50 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 MIC 50 of 1.5 mg/L, and exhibits higher potency when co-treats with Vancomycin (HY-B0671) with an MIC 50 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 EC 50 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 EC 50 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 EC 50 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 IC 50 s 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 × 10 8 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 × 10 6 CFU/lung) in the nasal infection model compared with control PBS (5.2 × 10 7 CFU/lung) mice.

Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT01821625 University of Texas Southwestern Medical Center|GlaxoSmithKline
Thrombocytopenia|Hepatitis C
April 2013 Phase 2|Phase 3
NCT03718533 Novartis Pharmaceuticals|Novartis
Poor Graft Function
December 17, 2018 Phase 2
NCT00442871 GlaxoSmithKline
Purpura, Thrombocytopaenic, Idiopathic
September 28, 2006 Phase 1

Appearance

Solid


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

  • 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

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


Synonyms

[1,1′-Biphenyl]-3-carboxylic acid, 3′-[(2Z)-2-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazinyl]-2′-hydroxy-, compd. with 2-aminoethanol (1:2)
[1,1′-Biphenyl]-3-carboxylic acid, 3′-[(2Z)-[1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2′-hydroxy-, compd. with 2-aminoethanol (1:2)
SB 497115GR
Eltrombopag olamine
Promacta
Eltrombopag diethanolamine salt
Revolade