| Description | DG-041 is an antagonist of high affinity EP3 receptor (IC50s: 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively ). DG-041 inhibits PGE2 facilitation of platelet aggregation and it also crosses the blood-brain barrier. |
| In vitro | DG-041作为DP1（IC50：131 nM）、EP1（IC50：486 nM）及TP受体（IC50：742 nM）的拮抗剂，其效果相对较弱[1]。 |
| In vivo | DG-041静脉注射的清除率为1250 mL/h/kg。对于静脉注射(i.v)或口服(p.o)，DG-041的剂量分别为1.78 mg/kg和9.62 mg/kg，其半衰期分别为2.7小时和4.06小时。同样，DG-041在静脉注射和口服给药时的最大浓度(Cmax)分别为9.46 μM和2.74 μM [1]。 |
| Target activity | EP3 receptor:4.6/8.1 nM |
| molecular weight | 592.32 |
| Molecular formula | C23H15Cl4FN2O3S2 |
| CAS | 861238-35-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/ml (92.86 mM), Sonication is recommended. |
| References | 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. |