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