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SQ 29,548 is a highly selective TP receptor antagonist which binds to the human recombinant TP receptor with a Ki of 4.1 nM.1 It inhibits the aggregation of washed human platelets induced by U-46619 with an IC50 of 0.06 µM.2 It antagonizes U-46619 induced contraction of rat and guinea pig tracheal, arterial, and venous smooth muscles with drug/receptor dissociation constants (KB) in the range of 0.5-1.7 nM.3 SQ 29,548 also inhibits the contraction of rat vascular smooth muscle induced by 8-iso PGF2α.4
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1. The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochim. Biophys. Acta 1483(2), 285-293 (2000).
2. Pharmacological actions of SQ 29,548, a novel selective thromboxane antagonist. J. Pharmacol. Exp. Ther. 234, 435-441 (1985).
3. Interspecies differences in thromboxane receptors: Studies with thromboxane receptor antagonists in rat and guinea pig smooth muscles. J. Pharmacol. Exp. Ther. 260, 789-794 (1992).
4. Evidence for the existence of F2-
Pharmacodynamic interplay of the P2Y1, P2Y12, and TXA2 pathways in platelets: The potential of triple antiplatelet therapy with P2Y1 receptor antagonism. Thromb. Res. 131(2), e64-e70 (2013).
Dual effect of isoprostanes on the release of [3H]D-
Pharmacological characterization of a novel antiglaucoma agent, bimatoprost (AGN 192024). J. Pharmacol. Exp. Ther. 305(2), 772-785 (2003).