TPalpha and TPbeta are two isoforms of the human TP receptor, the G protein-coupled receptor (GPCR) that mediates the actions of thromboxane A2 (TXA2). Although their distinct physiological functions have not been fully elucidated, TPbeta is believed to be responsible for vascular endothelial growth factor-induced endothelial cell differentiation and migration whereas TPalpha appears to be the predominant isoform expressed in platelets. CAY10535 is a TP receptor antagonist that shows ~20-fold selectivity for TPbeta (IC50 = 99 nM) relative to TPalpha (IC50 = 1,970 nM) in the inhibition of U46619-mediated Ca2+ mobilization. This compound exhibits relatively poor activity on platelets (IC50 = 985 nM) when inhibiting U-46619-induced platelet aggregation.
Molekulargewicht:
423.44
CAS Nummer:
[945716-28-9]
Formel:
C18H21N3O7S
Target-Kategorie:
Prostaglandin Receptor|||Others
T36550
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