711019-86-2

Solubility:Soluble to 100 mM in DMSO

Storage:at -20℃ 2 years

Biologieal

Selective antagonist of P2Y₆ nucleotide receptors; IC₅₀ values are 37 and 98 nM at human and rat P2Y₆ receptors respectively. Displays no activity at P2Y₁, P2Y₂, P2Y₄ and P2Y₁₁ receptors (IC₅₀ > 10 μM). Inhibits agonist-induced cardiomyocyte contraction and UDP-induced phagocytosis.
 

Reference

Mamedova et al (2004) Diisothiocyanate derivatives as potent, insurmountable antagonists of P2Y₆ nucleotide receptors. Biochem.Pharmacol. 67 1763. Wihlborg et al (2006) Positive inotropic effects by uridine triphosphate (UTP) and uridine diphosphate (UDP) via P2Y₂ and P2Y₆ receptors on cardiomyocytes and release of UTP in man during myocardial infarction. Circ.Res. 98 970. Koizumi et al (2007) UDP acting at P2Y₆ receptors is a mediator of microglial phagocytosis. Nature 446 1091.