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Eltrombopag Olamine

Cat. No. M4822
Eltrombopag Olamine Structure
Synonym:

Eltrombopag diethanolamine salt; SB-497115GR

Size Price Availability Quantity
10mM*1mL USD 120  USD120 In stock
10mg USD 90  USD90 In stock
50mg USD 200  USD200 In stock
100mg USD 280  USD280 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Eltrombopag (SB-497115-GR, Promacta, Revolade) is a small molecule agonist of the c-mpl (TpoR) receptor with an IC50 of 0.69 μM for the inhibition of hERG K+ channel tail current. In preclinical studies, the compound was shown to interact selectively with the thrombopoeitin receptor, leading to activation of the JAK-STAT signaling pathway and increased proliferation and differentiation of megakaryocytes. Animal studies confirmed that administration could increase platelet counts. In addition, eltrombopag (SB-497115-GR, Promacta, Revolade) decreased proliferation of all cancer cell lines.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 564.63
Formula C29H36N6O6
CAS Number 496775-62-3
Purity >98%
Solubility DMSO
Storage at -20°C
References

[1] Zhang Y, et al. Clin Ther. Eltrombopag: an oral thrombopoietin receptor agonist for the treatment of idiopathic thrombocytopenic purpura.

[2] Garnock-Jones KP. Drugs. Eltrombopag: a review of its use in treatment-refractory chronic primary immune thrombocytopenia.

[3] Cheng G. Expert Rev Hematol. Eltrombopag for the treatment of immune thrombocytopenia.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Eltrombopag Olamine, Eltrombopag diethanolamine salt; SB-497115GR supplier, Thrombopoietin/Thrombin, inhibitors

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