Quality Segment
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (warmed)
storage temp.
2-8°C
SMILES string
ClC1=CC(C(NC2=NC(C3=CC(Cl)=CS3)=C(N4CCN(C5CCCCC5)CC4)S2)=O)=CN=C1N6CCC(C(O)=O)CC6
Application
Biochem/physiol Actions
Avatrombopag (E5501; YM477; AKR 501) is an orally active, potent, and human and chimpanzee species-specific thrombopoietin (TPO) receptor (TPOR) agonist that induces cellular STAT3/5 phosphorylation and proliferation of hTPOR-expressing Ba/F3 cells (proliferation EC50 = 3.3 nM). Avatrombopag promotes megakaryocyte differentiation from human cord blood (CB) CD34+ cells (EC50 = 25 nM) and increases the number of human platelets in NOD/SCID mice transplanted with human fetal liver CD34(+) cells in vivo (0.3, 1, 3 mg/kg/d p.o.). This small molecule agonist of the TPO‐RA enhances platelet production by activating the receptor and mimicking the biological effects of thrombopoietin (TPO). Its distinctive chemical structure allows for selective binding to the transmembrane domain of the TPO receptor (TPO-R), preventing interference with the binding of endogenous TPO. Avatrombopag activates crucial intracellular pathways, such as the phosphorylation of STAT3, STAT5, and ERK (MAPK), which promote the differentiation and proliferation of megakaryocytes, a vital process for platelet production.
Orally active, potent and human and chimpanzee species-specific thrombopoietin receptor (TPO) agonist in vitro and in vivo.
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Skin Irrit. 2
存储类别
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable