CAY10535 Exclusive Property

storage temp. 

Store at -20°C

solubility 

DMF: 20 mg/ml; DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml; DMSO: 20 mg/ml; Ethanol: 10 mg/ml

form 

A crystalline solid

Hazard and Precautionary Statements (GHS)

CAY10535 Exclusive Chemical Properties,Usage,Production

Description

TPα and TPβ 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, TPβ is believed to be responsible for vascular endothelial growth factor-induced endothelial cell differentiation and migration whereas TPα appears to be the predominant isoform expressed in platelets. CAY10535 is a TP receptor antagonist that shows ~20-fold selectivity for TPβ (IC₅₀ = 99 nM) relative to TPα (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.¹

References

1. Hanson, J., Dogné, J.M., Ghiotto, J., et al. Design, synthesis, and SAR study of a series of N-alkyl-N'-[2-(aryloxy)-5-nitrobenzenesulfonyl]ureas and -cyanoguanidine as selective antagonists of the TPα and TPβ isoforms of the human thromboxane A₂ receptor J. Med. Chem. 50(16),3928-3936(2007).