DG 041

DG-041 is a potent, high affinity and selective EP3 receptor antagonist with IC50s of 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively. DG-041 inhibits PGE2 facilitation of platelet aggregation. DG-041 crosses the blood-brain barrier[1][2].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor

EP3 receptor:4.6-8.1 nM (IC50)

DG-041 was a less potent antagonist of the DP1 (IC50=131 nM), EP1 (IC50=486 nM), and TP receptors (IC50=742 nM)[1].

DG-041 (1.78 mg/kg for intravenous or 9.62 mg/kg for oral) has t1/2 of 2.7 hours, 4.06 hours and Cmax of 9.46 μM, 2.74 μM for intravenous and oral administration, respectively. DG-041 has CL of 1250 mL/h/kg for intravenous[1]. Animal Model: Male SpragueDawley rat[1] Dosage: 1.78 mg/kg (intravenous) or 9.62 mg/kg (oral) Administration: Intravenous or oral Result: Had t1/2 of 2.7 hours, 4.06 hours and Cmax of 9.46 μM, 2.74 μM for intravenous and oral administration, respectively.

[1]. Singh J, et al. Antagonists of the EP3 receptor for prostaglandin E2 are novel antiplatelet agents that do not prolong bleeding. ACS Chem Biol. 2009 Feb 20;4(2):115-26.

[2]. Hategan G, et al. Heterocyclic 1,7-disubstituted indole sulfonamides are potent and selective human EP3 receptorantagonists. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6797-800.