A thrombopoietin receptor agonist (EC50 = 0.27 µM) and iron chelator; It increases STAT5 phosphorylation in N2C-Tpo cells at 30 µM and p42/44 MAPK phosphorylation at 10 µM; stimulates megakaryocytopoiesis in human primary bone marrow cells; increases platelet production in chimpanzees at 10 mg/kg per day for five days; binds to iron (III) and mobilizes cellular iron and ferritin in H9C2

Eltrombopag – 5 mg

Brand:
Cayman
CAS:
496775-61-2
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Eltrombopag is an orally bioavailable nonpeptide agonist of the thrombopoietin receptor (EC50 = 0.27 µM in a reporter assay) and an iron chelator.{16951} It increases STAT5 phosphorylation in N2C-Tpo cells when used at a concentration of 30 µM and p42/44 MAPK phosphorylation when used at 10 µM. Eltrombopag binds to the transmembrane domain of the thrombopoietin receptor and stimulates megakaryocytopoiesis in human primary bone marrow cells. It increases platelet production in chimpanzees when administered at a dose of 10 mg/kg per day for five days. Eltrombopag also binds to iron (III) and mobilizes cellular iron and ferritin in H9C2, Huh7, and RINm5F cells in a concentration-dependent manner.{47035} It enhances cellular iron mobilization when used in combination with the iron chelators deferasirox (Item No. 16753) and CP40.  

 

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Description

A thrombopoietin receptor agonist (EC50 = 0.27 µM) and iron chelator; It increases STAT5 phosphorylation in N2C-Tpo cells at 30 µM and p42/44 MAPK phosphorylation at 10 µM; stimulates megakaryocytopoiesis in human primary bone marrow cells; increases platelet production in chimpanzees at 10 mg/kg per day for five days; binds to iron (III) and mobilizes cellular iron and ferritin in H9C2, Huh7, and RINm5F cells

Formal name: 3’-[2-[(2Z)-1-(3,4-dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazinyl]-2’-hydroxy-[1,1’-biphenyl]-3-carboxylic acid

Synonyms:  SB 497115

Molecular weight: 442.5

CAS: 496775-61-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cardiovascular System|Blood|Acute Phase Reactants||Research Area|Immunology & Inflammation|Innate Immunity

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