Sitaxsentan

CAS No. 184036-34-8

Sitaxsentan( IPI-1040 | Sitaxentan | TBC-11251 )

Catalog No. M12843 CAS No. 184036-34-8

A potent, long acting, orally active, selective ETA receptor antagonist that binds competitively to human ETA receptor with Ki of 0.43 nM, IC50 of 1.4 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Sitaxsentan
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, long acting, orally active, selective ETA receptor antagonist that binds competitively to human ETA receptor with Ki of 0.43 nM, IC50 of 1.4 nM.
  • Description
    A potent, long acting, orally active, selective ETA receptor antagonist that binds competitively to human ETA receptor with Ki of 0.43 nM, IC50 of 1.4 nM; dispalys >5,000-fold selectivity over ETB receptors; inhibits ET1-induced stimulation of phosphoinositide turnover with Ki of 0.686 nM, and pA2 of 8.0; excellent PK profile and oral bioavailability.Hypertension Withdrawn.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    IPI-1040 | Sitaxentan | TBC-11251
  • Pathway
    GPCR/G Protein
  • Target
    Endothelin Receptor
  • Recptor
    Endothelin Receptor
  • Research Area
    Cardiovascular Disease
  • Indication
    Hypertension

Chemical Information

  • CAS Number
    184036-34-8
  • Formula Weight
    454.9045
  • Molecular Formula
    C18H15ClN2O6S2
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    CC1=CC2=C(C=C1CC(=O)C3=C(C=CS3)S(=O)(=O)NC4=C(C(=NO4)C)Cl)OCO2
  • Chemical Name
    3-Thiophenesulfonamide, N-(4-chloro-3-methyl-5-isoxazolyl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Wu C, et al. J Med Chem. 1997 May 23;40(11):1690-7. 2. Wanebo JE, et al. Neurosurgery. 1998 Dec;43(6):1409-17; discussion 1417-8. 3. Tilton RG, et al. Pulm Pharmacol Ther. 2000;13(2):87-97.
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