861238-35-9

Basic information

• Product Name: DG-041
• Synonyms: DG-041;(E)-3-[1-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methylindol-7-yl]-N-(4,5-dichlorothiophen-2-yl)sulfonylprop-2-enamide
• CAS NO: 861238-35-9
• Molecular Formula: C23H15Cl4FN2O3S2
• Molecular Weight: 592.32
• Mol File: 861238-35-9.mol
• Article Data: 5

Chemical Properties

• Melting Point: 236-238 °C
• Appearance: /
• Density: 1.57±0.1 g/cm3(Predicted)
• PKA: 3.55±0.10(Predicted)
• CAS DataBase Reference: DG-041(CAS DataBase Reference)
• NIST Chemistry Reference: DG-041(861238-35-9)
• EPA Substance Registry System: DG-041(861238-35-9)

Safety Data

• Hazardous Substances Data: 861238-35-9(Hazardous Substances Data)

Usage

General Description

DG-041 is a small molecule drug that acts as a potent and selective antagonist of the protease-activated receptor 1 (PAR-1). It has been studied for its potential therapeutic benefits in conditions such as atherosclerosis, thrombosis, and inflammation. By blocking the activation of PAR-1, DG-041 has been shown to inhibit platelet aggregation and reduce the risk of thrombotic events. Additionally, it has demonstrated anti-inflammatory properties by inhibiting the expression of pro-inflammatory mediators. DG-041 shows promise as a potential treatment for cardiovascular and inflammatory diseases, and further research is ongoing to explore its clinical applications.

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Relevant articles and documents

Structure - activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4, 5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor antagonist, as a novel antiplatelet agent that does not prolong bleeding

The EP3 receptor on the platelet mediates prostaglandin E 2 potentiation of thrombogenic coagonists including collagen and adenosine diphosphate (ADP). A pharmacophore driven approach led to the identification of diverse peri-substituted heterocycles as potent and selective EP3 receptor antagonists. A simultaneous chemical optimization and druglike assessment of prioritized molecules converged on a lead compound 50 (DG-041) that displayed favorable in vitro and functional activities as an inhibitor of human platelet aggregation. This agent is currently in human clinical trials for the treatment of atherothrombosis.

7-(ACRYLOYL) INDOLE COMPOSITIONS AND METHODS FOR MAKING AND USING SAME

The present invention is directed to pharmaceutical compositions of 7-(acryloyl) indoles, such as 4,5-Dichloro-thiophene-2-sulfonic acid [(E)-3-[1-(2,4-dichlorophenylmethyl)-5-fluoro-3-methyl-1H-indol-7-yl]-acryloyl]amide (DTSI). The invention is also dir

Sulfonamide peri-substituted bicyclics for occlusive artery disease

Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representative example is: