Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells at 3 uM measured after 15 mins by flow cytometric analysis
Antagonist activity at human P2Y6R expressed in human 1321N1 cells assessed as inhibition of UDP-induced calcium mobilization at 10 uM preincubated for 30 mins followed by UDP addition measured after 1 hr by FLIPR assay
Antagonist activity at human P2Y1R expressed in human 1321N1 cells assessed as inhibition of MeSADP-induced calcium mobilization at 10 uM preincubated for 30 mins followed by MeSADP addition measured after 1 hr by FLIPR assay
Antagonist activity at human P2Y1R expressed in human 1321N1 cells assessed as inhibition of 2-MeSADP-mediated calcium mobilization at 10 uM by PDSP assay
Antagonist activity at PAR1 (unknown origin) expressed in mouse KOLF cells assessed as inhibition of TRAP-induced calcium mobilization at 10 uM by PDSP assay
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
Antagonist activity at human P2Y14R expressed in CHO cells assessed as inhibition of UDPG-mediated reduction of forskolin-induced cAMP production at 1 uM after 15 mins by by competitive enzyme-linked immunoassay
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
Antinociceptive activity in ip dosed ICR mouse model of chronic constriction injury-induced neuropathic pain assessed as inhibition of mechanical allodynia administered 7 days post-surgery and measured after 1 hr post-dose by Von Frey assay