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Eltrombopag Olamine

Cat. No. M4822
Eltrombopag Olamine Structure
Synonym:

Eltrombopag diethanolamine salt; SB-497115GR

Size Price Availability Quantity
10mM*1mL in DMSO USD 100  USD100 In stock
10mg USD 90  USD90 In stock
50mg USD 225  USD225 In stock
100mg USD 290  USD290 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 564.63
Formula C29H36N6O6
CAS Number 496775-62-3
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

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


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