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. 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. NF449 has also demonstrated selective antagonism of the Gsα-subunit G protein, which suppresses the association rate of GTPγS binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks G protein coupling to certain GPCRs.
