An EP3 receptor antagonist
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DG-041

Item No. 13234

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-3-[1-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-1H-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide
CAS Number
861238-35-9
Molecular Formula
C23H15Cl4FN2O3S2
Formula Weight
592.3
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
CC1=CN(CC2=C(Cl)C=C(Cl)C=C2)C3=C1C=C(F)C=C3/C=C/C(NS(C4=CC(Cl)=C(Cl)S4)(=O)=O)=O
InChi Code
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+
InChi Key
BFBTVZNKWXWKNZ-HWKANZROSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $93

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    10 mg

    $176

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    25 mg

    $416

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    50 mg

    $740

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    Product Description

    DG-041 is an antagonist of the prostaglandin E2 (PGE2; Item No. 14010) receptor subtype EP3 (IC50 = 8.1 nM in a calcium mobilization assay).1 It is selective for EP3 over DP1, EP1, and TP receptors (IC50s = 131, 486, and 742 nM, respectively, in calcium mobilization assays) as well as EP2, EP4, IP, FP, and DP2/CRTH2 receptors (IC50s = >10,000 nM for all in calcium mobilization assays). DG-041 (1 µM) inhibits collagen- and PGE2-induced platelet aggregation in isolated rat platelets. It inhibits P-selectin expression induced by the TP receptor agonist U-46619 (Item No. 16450) in isolated and washed human platelets when used at a concentration of 3 µM.2 DG-041 (10 or 100 mg/kg) inhibits collagen- and PGE2-induced platelet aggregation in rat platelet-rich plasma ex vivo without increasing bleeding time in the same rats.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Singh, J., Zeller, W., Zhou, N., et al. Antagonists of the EP3 receptor for prostaglandin E2 are novel antiplatelet agents that do not prolong bleeding. ACS Chem. Biol. 4(2), 115-126 (2009).

    2. Heptinstall, S., Espinosa, D.I., Manolopoulos, P., et al. DG-041 inhibits the EP3 prostanoid receptor—a new target for inhibition of platelet function in atherothrombotic disease. Platelets 19(8), 605-613 (2008).