TABLE 1

Comparison of the activities of AR-C compounds on constitutively activated P2Y12 chimera stably expressed in CHO-K1 cells cAMP assays were performed in the presence of 20 μM forskolin as described under Materials and Methods. Inhibition of phosphorylated Akt (pAkt) was compared with control through densitometric analysis of the Western blots. Data are expressed as mean ± S.E.M. representing at least three separate experiments.

cAMP Conversion from ATP (×103) Inhibition of pAkt
%
Control 26.7 ± 2.9 0
AR-C78511 100 nM 88 ± 12 76 ± 9
AR-C69931MX 300 nM 27.8 ± 4 9.7 ± 2.4
AR-C66096 3 μM 40 ± 6 44 ± 5
AR-C67085 1 μM 48 ± 6 24 ± 4
AR-C69581 3 μM 44 ± 4 17 ± 4