Aprocitentan

• Description :

  Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent[1].

• Product Name Alternative :

  ACT-132577

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  Endothelin Receptor

• Type :

  Reference compound

• Related Pathways :

  GPCR/G Protein

• Applications :

  COVID-19-immunoregulation

• Field of Research :

  Cardiovascular Disease; Endocrinology

• Assay Protocol :

  https://www.medchemexpress.com/ACT-132577.html

• Purity :

  99.55

• Solubility :

  DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

• Smiles :

  O=S(N)(NC1=NC=NC(OCCOC2=NC=C(Br)C=N2)=C1C3=CC=C(Br)C=C3)=O

• Molecular Formula :

  C16H14Br2N6O4S

• Molecular Weight :

  546.19

• Precautions :

  H302, H315, H319, H335

• References & Citations :

  [1]Iglarz M, et al. Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist. J Pharmacol Exp Ther. 2008 Dec;327 (3) :736-45.|[2]Zhang J, et al. Pharmacokinetic study of ACT-132577 in rat plasma by ultra performance liquid chromatography-tandem mass spectrometry. Int J Clin Exp Med. 2015 Oct 15;8 (10) :18420-6

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Launched

• Isoform :

  ETA; ETB

• CAS Number :

  [1103522-45-7]