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861238-35-9

861238-35-9 structure
861238-35-9 structure
  • Name: DG 041
  • Chemical Name: 3-[1-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methylindol-7-yl]-N-(4,5-dichlorothiophen-2-yl)sulfonylprop-2-enamide
  • CAS Number: 861238-35-9
  • Molecular Formula: C23H15Cl4FN2O3S2
  • Molecular Weight: 592.31700
  • Catalog: Signaling Pathways GPCR/G Protein Prostaglandin Receptor
  • Create Date: 2017-11-20 10:25:02
  • Modify Date: 2024-01-09 10:04:47
  • 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].

Name 3-[1-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methylindol-7-yl]-N-(4,5-dichlorothiophen-2-yl)sulfonylprop-2-enamide
Description 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].
Related Catalog
Target

EP3 receptor:4.6-8.1 nM (IC50)

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

Molecular Formula C23H15Cl4FN2O3S2
Molecular Weight 592.31700
Exact Mass 589.92600
PSA 108.28000
LogP 9.25160
Storage condition 2-8°C