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DG-041

Catalog No. T15108 CAS 861238-35-9

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.

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DG-041, CAS 861238-35-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 43.00
2 mg	In stock	$ 61.00
5 mg	In stock	$ 98.00
10 mg	In stock	$ 162.00
25 mg	In stock	$ 316.00
50 mg	In stock	$ 568.00
100 mg	In stock	$ 818.00
500 mg	In stock	$ 1,690.00
1 mL * 10 mM (in DMSO)	In stock	$ 112.00

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Biological Description

Chemical Properties

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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.
Targets&IC50	EP3 receptor:4.6/8.1 nM
In vitro	DG-041 was a less effective the DP1 (IC50: 131 nM), EP1 (IC50: 486 nM) and TP receptors (IC50: 742 nM) antagonist [1].
In vivo	DG-041 has CL of 1250 mL/h/kg for intravenous. DG-041 (1.78 mg/kg for i.v or 9.62 mg/kg for p.o) has t1/2 of 2.7 hours, 4.06 hours. DG-041 (1.78 mg/kg for i.v or 9.62 mg/kg for p.o) has Cmax of 9.46 μM, 2.74 μM for intravenous and oral administration, respectively [1].

Molecular Weight	592.32
Formula	C23H15Cl4FN2O3S2
CAS No.	861238-35-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/ml (92.86 mM), Sonication is recommended.

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Inhibitor Library Membrane Protein-targeted Compound Library Bioactive Compound Library Bioactive Compounds Library Max ReFRAME Related Library

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Keywords

DG-041 861238-35-9 GPCR/G Protein Immunology/Inflammation Prostaglandin Receptor barrier blood-brain Inhibitor inhibit DG 041 infarction stroke plaque DG041 atherothrombosis atherosclerotic Myocardial inhibitor

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