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Aprocitentan

CHEMBL2165326 Phase 4 已批准 Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
546.2 g/mol
LogP
2.4
Phase
4

A dual endothelin receptor antagonist that blocks both ETA and ETB receptors to relax blood vessels and lower blood pressure in patients with resistant hypertension. It represents a new mechanism for treating hard-to-control high blood pressure.

分子量

546.2000 g/mol

LogP

2.40

TPSA

151.00 Ų

Lipinski 五规则

符合

治疗领域

Hypertension

作用机制

Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

机制

Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.

二维结构

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
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SMILES

                    
NS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1

                

                

                
                

                    
InChI

                    
InChI=1S/C16H14Br2N6O4S/c17-11-3-1-10(2-4-11)13-14(24-29(19,25)26)22-9-23-15(13)27-5-6-28-16-20-7-12(18)8-21-16/h1-4,7-9H,5-6H2,(H2,19,25,26)(H,22,23,24)

                

                

                

                    
                    

                        
Molecular Formula

                        
C16H14Br2N6O4S

                    

                    
                    

                        
HBD / HBA

                        
2 / 10

                    

                    
                    

                        
可旋转键数

                        
8

                    

                    
                    
                    

                        
重原子数

                        
29

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
No targets recorded

    
    
Target interaction data is not yet available for this drug.

    



                
            


            
            

                
                


    
    
        
    
    
    
No interactions recorded

    
    
Drug interaction data is not yet available for this compound.

    



                
            


            
            

                
                


    
    
        
    
    
    
No side effects recorded

    
    
Side effect data is not yet available for this drug.

    



                
            


            
            
            

                
常见问题

                

                    
                    

                        
                        

                            
A dual endothelin receptor antagonist that blocks both ETA and ETB receptors to relax blood vessels and lower blood pressure in patients with resistant hypertension. It represents a new mechanism for treating hard-to-control high blood pressure.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Aprocitentan is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.

                        

                    

                

            

            

            
            

            
            

            
            
{# References & Data Sources section for drug detail pages.
   Renders standard pharmacological database links plus the drug's data_sources field. #}


    
References & Data Sources

    
    
        
        
  • 
            
            
                ChEMBL — European Bioinformatics Institute (EBI).
                CHEMBL2165326.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 25099191.
                Chemical information database.
            
        
    • 
        
        
        
        
    

    
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.




        


        
        
    


    



    
医疗免责声明

    

        This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.
    

    

        Data sources:
        ChEMBL,
        PubChem,
        DailyMed.