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Merck
CN

SML4197

Eltrombopag olamine

new

≥98% (HPLC)

Synonym(s):

3′-[(2Z)-2-[1-(3,4-Dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazinyl]-2′-hydroxy[1,1′-biphenyl]-3-carboxylic acid, bis-(monoethanolamine), (Z)-3′-(2-(1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)-2′-hydroxybiphenyl-3-carboxylic acid, bis-(monoethanolamine), SB 497115 bis-(ethanolamine) salt, SB-497115 bis-(ethanolamine) salt, SB497115 bis-(ethanolamine) salt

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Quality Level

100

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

light brown-red to very dark brown-red

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Biochem/physiol Actions

Orally active, potent and selective thrombopoietin (Tpo) receptor (TpoR) agonist in vitro and in vivo.
Eltrombopag is an orally active nonpeptide thrombopoietin receptor (TpoR) agonist that selectively induces STAT activation and proliferation (EC50 = 270 & 30 nM, respectively) of hToR-transfected, but not non-transfected, BAF3 cells. Eltrombopag increases the differentiation of primary human CD34(+) bone marrow cells into CD41(+) megakaryocytes ex vivo (EC50 = 100 nM) and exhibits thrombopoietic activity in chimpanzees in vivo (10 mg/kg/day p.o.).

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Certificates of Analysis (COA)

Lot/Batch Number
0000482570
0000482573
0000475863
0000475863

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Darren Kelly et al.
Journal of veterinary internal medicine, 34(2), 890-892 (2020-02-26)
Idiopathic aplastic pancytopenia is an uncommon disease in dogs which results in pancytopenia and for which an immune-mediated etiology is suspected. A small number of affected dogs reported in the veterinary literature have responded to immunosuppressive medication but the prognosis
Eltrombopag inhibits the proliferation of Ewing sarcoma cells via iron chelation and impaired DNA replication
Waters T, et al.
BMC Cancer, 20 (2020)
Gavin C Sampey et al.
Viruses, 12(10) (2020-09-27)
Human immunodeficiency virus 1 (HIV-1) is the most prevalent human retrovirus. Recent data show that 34 million people are living with HIV-1 worldwide. HIV-1 infections can lead to AIDS which still causes nearly 20,000 deaths annually in the USA alone.
Francesco D'Alò et al.
Platelets, 32(3), 378-382 (2020-04-10)
Thrombocytopenia is a severe complication for patients with myelodysplastic syndrome (MDS). Eltrombopag increases platelet count in MDS patients but its combination with azacitidine elicited controversial results. We aimed to quantify the colony forming units of megakaryocytes (CFU-Mk) obtained from CD34+ bone
Grace Nevil et al.
Pediatric hematology and oncology, 38(1), 8-13 (2020-08-18)
Eltrombopag is a small molecule, thrombopoietin receptor agonist approved for the treatment of patients with aplastic anemia and chronic immune thrombocytopenia. It is also a polyvalent cation chelator and inhibits leukemia cell proliferation via reduction of intracellular iron. The in vivo
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