NF449 (sodium salt)

NF449 is an analog of suramin that selectively inhibits P2X1 purinergic receptors (pIC50 = 6.3) with a potency 19-fold greater than at P2X3, P2Y1, P2Y2, or P2Y11.{23042,23041} Through selective inhibition of the P2X1 receptor, 10 mg/kg NF449 has been used to decrease intravascular platelet aggregation in a mouse model of systemic thromboembolism.{23040} NF449 has also demonstrated selective antagonism of the Gs?-subunit G protein, which suppresses the association rate of GTP?S binding to Gs?-s, inhibits the stimulation of adenylyl cyclase activity, and blocks G protein coupling to certain GPCRs.{23039}