1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. DG-041

DG-041 

Cat. No.: HY-10835
Handling Instructions

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.

For research use only. We do not sell to patients.

DG-041 Chemical Structure

DG-041 Chemical Structure

CAS No. : 861238-35-9

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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].

IC50 & Target[1]

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.
Molecular Weight

592.32

Formula

C₂₃H₁₅Cl₄FN₂O₃S₂

CAS No.

861238-35-9

SMILES

O=C(NS(=O)(C1=CC(Cl)=C(Cl)S1)=O)/C=C/C2=CC(F)=CC3=C2N(CC4=CC=C(Cl)C=C4Cl)C=C3C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

DG-041DG041DG 041Prostaglandin Receptorblood-brainbarrierMyocardialinfarctionstrokeatheroscleroticplaqueatherothrombosisInhibitorinhibitorinhibit

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DG-041
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HY-10835
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