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Home - Products - Proteasome/Ubiquitin - Endogenous Metabolite - Aprocitentan

Aprocitentan

CAS No. 1103522-45-7

Aprocitentan( ACT-132577 )

Catalog No. M21083 CAS No. 1103522-45-7

Aprocitentan is ETA and ETB antagonist .

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Aprocitentan
  • Note
    Research use only, not for human use.
  • Brief Description
    Aprocitentan is ETA and ETB antagonist .
  • Description
    Aprocitentan is ETA and ETB antagonist .(In Vitro):Aprocitentan (ACT-132577) achieves full inhibition of intracellular calcium increase induced by ET-1 on nonrecombinant cells (primary human pulmonary smooth muscle cells and rat aortic smooth muscle cell line A10 and mouse fibroblast cell line 3T3).(In Vivo):Aprocitentan (ACT-132577) has a volume of distribution greater than the plasma volume and a longer half-life than its parent compound in the rat. In rat plasma, the mean recovery of Aprocitentan (ACT-132577) ranges from 82.6% to 90.6%, matrix effect of Aprocitentan (ACT-132577) in rat plasma ranges from 101.4% to 115.2%.
  • In Vitro
    Aprocitentan (ACT-132577) achieves full inhibition of intracellular calcium increase induced by ET-1 on nonrecombinant cells (primary human pulmonary smooth muscle cells and rat aortic smooth muscle cell line A10 and mouse fibroblast cell line 3T3).
  • In Vivo
    Aprocitentan (ACT-132577) has a volume of distribution greater than the plasma volume and a longer half-life than its parent compound in the rat. In rat plasma, the mean recovery of Aprocitentan (ACT-132577) ranges from 82.6% to 90.6%, matrix effect of Aprocitentan (ACT-132577) in rat plasma ranges from 101.4% to 115.2%.
  • Synonyms
    ACT-132577
  • Pathway
    Proteasome/Ubiquitin
  • Target
    Endogenous Metabolite
  • Recptor
    ET-A |ET-B
  • Research Area
    Cardiovascular Disease
  • Indication
    Resistant Hypertension

Chemical Information

  • CAS Number
    1103522-45-7
  • Formula Weight
    546.19
  • Molecular Formula
    C16H14Br2N6O4S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:46 mg/mL (84.22 mM)
  • SMILES
    NS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1
  • Chemical Name
    N-[5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl]sulfuric diamide

Shipping & Storage Information

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

Reference

1.Trensz F Bortolamiol C Kramberg M et al. Journal of Pharmacology & Experimental Therapeutics 2019.
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