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Chemical Structure| 861238-35-9 Chemical Structure| 861238-35-9

Structure of DG-041
CAS No.: 861238-35-9

Chemical Structure| 861238-35-9

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DG-041 is a potent and selective antagonist of prostanoid EP3 receptor with IC50 of 4.6 nM.

Synonyms: DG-041

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Product Details of DG-041

CAS No. :861238-35-9
Formula : C23H15Cl4FN2O3S2
M.W : 592.32
SMILES Code : 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
Synonyms :
DG-041
MDL No. :MFCD18251534

Safety of DG-041

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of DG-041

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
human platelets 1 μM EP3 antagonist DG-041 converted platelets of nonresponders to a PGE2-responsive phenotype Thromb Res. 2010 Jul;126(1):e23-9
LVIP2.0Zc cells 0.1 nM – 10 nM 6 h DG-041 was found to be a high-affinity, functional antagonist of the mouse EP3 γ receptor. Prostaglandins Other Lipid Mediat. 2019 Oct;144:106353
human islet β-cells 30 nM 4 days To assess the effect of DG-041 on human islet β-cell proliferation, results showed that blocking EP3 increased human β-cell proliferation. Mol Metab. 2017 Apr 5;6(6):548-559
mouse islet β-cells 30 nM 4 days To assess the effect of DG-041 on mouse islet β-cell proliferation, results showed that blockade of EP3 enhanced β-cell proliferation in young, but not old, mouse islets. Mol Metab. 2017 Apr 5;6(6):548-559
vascular smooth muscle cells 0.1-10 μmol/L 30 min DG-041 dose-dependently inhibited AngII-induced intracellular Ca2+ increase Arterioscler Thromb Vasc Biol. 2012 Dec;32(12):3024-32
vascular smooth muscle cells 1 µM 30 min DG-041 inhibited AngII-induced phosphorylation of MLC20 and MYPT1 Arterioscler Thromb Vasc Biol. 2012 Dec;32(12):3024-32

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Male C57BL/6 mice Diet-induced obesity model Subcutaneous injection 20 mg/kg Twice daily for one week DG-041 treatment effectively blocked the EP3 receptor and decreased skeletal muscle triglyceride content but had no significant effects on the diabetic phenotype. Prostaglandins Other Lipid Mediat. 2019 Oct;144:106353

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.69mL

0.34mL

0.17mL

8.44mL

1.69mL

0.84mL

16.88mL

3.38mL

1.69mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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