loader
Please Wait
Applying Filters...
Close
4

Bora CDMO Bora CDMO

X
menu

    Market Place

    Market Place

    Post Enquiry

    Post Enquiry
    menu

    Technical details about Sparsentan, learn more about the structure, uses, toxicity, action, side effects and more

    Client Email Product
    Menu

    Sparsentan

    APIs // Active Pharmaceutical Ingredients

    DEVELOPMENTS

    DOSSIERs // Finished Dosage Forms

    MARKET PLACE

    PATENTS

    DIGITAL CONTENT

    PharmaCompass

    PharmaCompass Sponsored Ads

    Athena Pharmaceutiques is a Partner of Choice for Drug Delivery & Life Cycle Management.

    2D Structure
    Also known as: 254740-64-2, Sparsentan (re-021), Re-021, Sparsentan [usan], Ps433540, Ps-433540
    Molecular Formula
    C32H40N4O5S
    Molecular Weight
    592.8  g/mol
    InChI Key
    WRFHGDPIDHPWIQ-UHFFFAOYSA-N
    FDA UNII
    9242RO5URM
    Sparsentan has been used in trials studying the treatment of Focal Segmental Glomerulosclerosis. Sparsentan is the first and only dual-acting angiotensin and endothelin receptor antagonist (DARA) in development.
    1 2D Structure

    2D Structure

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    2-[4-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-2-(ethoxymethyl)phenyl]-N-(4,5-dimethyl-1,2-oxazol-3-yl)benzenesulfonamide
    2.1.2 InChI
    InChI=1S/C32H40N4O5S/c1-5-7-14-29-33-32(17-10-11-18-32)31(37)36(29)20-24-15-16-26(25(19-24)21-40-6-2)27-12-8-9-13-28(27)42(38,39)35-30-22(3)23(4)41-34-30/h8-9,12-13,15-16,19H,5-7,10-11,14,17-18,20-21H2,1-4H3,(H,34,35)
    2.1.3 InChI Key
    WRFHGDPIDHPWIQ-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    CCCCC1=NC2(CCCC2)C(=O)N1CC3=CC(=C(C=C3)C4=CC=CC=C4S(=O)(=O)NC5=NOC(=C5C)C)COCC
    2.2 Other Identifiers
    2.2.1 UNII
    9242RO5URM
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. (1,1'-biphenyl)-2-sulfonamide, 4'-((2-butyl-4-oxo-1,3-diazaspiro(4.4)non-1-en-3-yl)methyl)-n-(4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-

    2. 4'-((2-butyl-4-oxo-1,3-diazaspiro(4.4)non-1-en-3-yl)methyl)-n-(4,5-dimethyl-1,2-oxazol-3-yl)-2'-(ethoxymethyl)-2-biphenylsulfonamide

    3. 4'-((2-butyl-4-oxo-1,3-diazaspiro(4.4)non-1-en-3-yl)methyl)-n-(4,5-dimethyl-1,2-oxazol-3-yl)-2'-(ethoxymethyl)biphenyl-2-sulfonamide

    4. Re-021

    2.3.2 Depositor-Supplied Synonyms

    1. 254740-64-2

    2. Sparsentan (re-021)

    3. Re-021

    4. Sparsentan [usan]

    5. Ps433540

    6. Ps-433540

    7. 9242ro5urm

    8. Chembl539423

    9. 2-[4-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-2-(ethoxymethyl)phenyl]-n-(4,5-dimethyl-1,2-oxazol-3-yl)benzenesulfonamide

    10. 4'-((2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl)-n-(4,5-dimethylisoxazol-3-yl)-2'-(ethoxymethyl)-[1,1'-biphenyl]-2-sulfonamide

    11. Retrophin

    12. (1,1'-biphenyl)-2-sulfonamide, 4'-((2-butyl-4-oxo-1,3-diazaspiro(4.4)non-1-en-3-yl)methyl)-n-(4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-

    13. [1,1'-biphenyl]-2-sulfonamide, 4'-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-n-(4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-

    14. Unii-9242ro5urm

    15. Dara

    16. Compound 7 [pmid 15634011]

    17. Dara-a

    18. Ps 33540

    19. Sparsentan [inn]

    20. Sparsentan (usan/inn)

    21. Sparsentan(ps433540)

    22. Sparsentan [who-dd]

    23. Schembl535109

    24. Gtpl8448

    25. Amy38147

    26. Bcp23969

    27. Ex-a3048

    28. Bdbm50175523

    29. S6665

    30. Cs-7947

    31. Db12548

    32. Sb16876

    33. Dara-a (dual Acting Receptor Antagonist Of Angiotension And Endothelin Receptors)

    34. Ps-433540;re-021;dara

    35. Ac-35179

    36. Hy-17621

    37. Sparsentan (ps-433540,re-021,dara)

    38. D11776

    39. F77045

    40. A858308

    41. L023324

    42. Q27088845

    43. 4''''-(2-butyl-4-oxo-1,3-diaza-spiro[4.4]non-1-en-3-ylmethyl)-2''''-ethoxymethyl-biphenyl-2-sulfonic Acid (4,5-dimethyl-isoxazol-3-yl)-amide

    44. 4''-(2-butyl-4-oxo-1,3-diaza-spiro[4.4]non-1-en-3-ylmethyl)-2''-ethoxymethyl-biphenyl-2-sulfonic Acid (4,5-dimethyl-isoxazol-3-yl)-amide

    45. 4'-((2-butyl-4-oxo-1,3-diazaspiro(4.4)non-1-en-3-yl)methyi)-n-(4,5- Dimethylisoxazol-3-yl)-2'-(ethoxymethyl)biphenyl-2-sulfonamide

    46. 4'-((2-butyl-4-oxo-1,3-diazaspiro(4.4)non-1-en-3-yl)methyl)-n-(4,5-dimethyl-1,2-oxazol-3-yl)-2'-(ethoxymethyl)-2-biphenylsulfonamide

    47. 4'-((2-butyl-4-oxo-1,3-diazaspiro(4.4)non-1-en-3-yl)methyl)-n-(4,5-dimethyl-1,2-oxazol-3-yl)-2'-(ethoxymethyl)biphenyl-2-sulfonamide

    2.4 Create Date
    2006-10-25
    3 Chemical and Physical Properties
    Molecular Weight 592.8 g/mol
    Molecular Formula C32H40N4O5S
    XLogP35
    Hydrogen Bond Donor Count1
    Hydrogen Bond Acceptor Count8
    Rotatable Bond Count12
    Exact Mass592.27194156 g/mol
    Monoisotopic Mass592.27194156 g/mol
    Topological Polar Surface Area123 Ų
    Heavy Atom Count42
    Formal Charge0
    Complexity1060
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Indication

    Treatment of focal segmental glomerulosclerosis

    Treatment of primary IgA nephropathy

    5 Pharmacology and Biochemistry
    5.1 Mechanism of Action

    Sparsentan, which possesses two clinically validated mechanisms of action in a single molecule, works by selectively blocking the action of two potent vasoconstrictor and mitogenic agents, angiotensin II (AII) and endothelin 1 (ET1), at their respective receptors. Sparsentan is highly selective (10,000-fold) for the AII receptor sub-type 1 and the ET receptor sub-type A. As such, Sparsentan combines the properties of an angiotensin receptor blocker (ARB) and an endothelin receptor antagonist (ERA) in the same molecule.

    Post Enquiry
    POST ENQUIRY