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Eltrombopag | Small molecule thrombopoietin agonist

CAS:
496775-61-2
Catalog Number:
10-3768
Activity:
Small molecule thrombopoietin agonist
Chemical 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
Alternate Name:
SB-497115
Molecular Weight:
442.47
Molecular Formula:
C25H22N4O4
Solubility:
Soluble in DMSO (up to 55 mg/ml) or in ethanol (up to 14 mg/ml).
Physical Properties:
Orange solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
Shipping Code:
RT

Eltrombopag (496775-61-2) is a novel, orally active, small molecule human thrombopoietin receptor (TPO-R) agonist, EC50=0.27 μM.1,2 Maintains human hematopoietic stem and progenitor cells under inflammatory conditions.3 Promotes DNA repair in human hematopoietic stem and progenitor cells.4 Acts as a powerful chelator of cellular and extracellular iron(III).5 Stimulates hematopoietic stem cells via a TPO-R-independent mechanism involving iron chelation.6

References/Citations:

1) Xie et al. (2018), Pharmacological characterization of eltrombopag, a novel orally active human thrombopoietin receptor agonist; J. Cell. Mol. Med., 22 5367
2) Erickson-Miller et al. (2008), Preclinical activity of eltrombopag (SB-497115), an oral, nonpeptide thrombopoietin receptor agonist; Stem Cells, 27 424
3) Alvarado et al. (2019), Eltrombopag maintains human hematopoietic stem and progenitor cells under inflammatory conditions mediated by IFN-γ; Blood, 133 2043
4) Guenther et al. (2019), Eltrombopag promotes DNA repair in human hematopoietic stem and progenitor cells; Exp. Hematol. 73 1
5) Vlachodimitropoulou et al. (2017), Eltrombopag: a powerful chelator of cellular or extracellular iron (II) alone or combined with a second chelator; Blood, 130 1923
6) Kao et al. (2018), Thrombopoietin receptor-independent stimulation of hematopoietic stem cells by eltrombopag; Science Transl. Med., 10 eaas9563

Eltrombopag | Small molecule thrombopoietin agonist is also available in the Cellular Metabolism Library.
CAS:
496775-61-2
Catalog Number:
10-3768
Activity:
Small molecule thrombopoietin agonist
Chemical 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
Alternate Name:
SB-497115
Molecular Weight:
442.47
Molecular Formula:
C25H22N4O4
Solubility:
Soluble in DMSO (up to 55 mg/ml) or in ethanol (up to 14 mg/ml).
Physical Properties:
Orange solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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