For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I006471 |
| CAS Number | 861238-35-9 |
| Synonyms | (E)-3-[1-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methylindol-7-yl]-N-(4,5-dichlorothiophen-2-yl)sulfonylprop-2-enamide |
| Molecular Formula | C23H15Cl4FN2O3S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C23H15Cl4FN2O3S2/c1-12-10-30(11-14-2-4-15(24)7-18(14)25)22-13(6-16(28)8-17(12)22)3-5-20(31)29-35(32,33)21-9-19(26)23(27)34-21/h2-10H,11H2,1H3,(H,29,31)/b5-3+ |
| InChIKey | BFBTVZNKWXWKNZ-HWKANZROSA-N |
| SMILES | CC1=CN(C2=C(C=C(C=C12)F)C=CC(=O)NS(=O)(=O)C3=CC(=C(S3)Cl)Cl)CC4=C(C=C(C=C4)Cl)Cl |
| Reference | [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. |
