Aprocitentan

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 Specifications

CAS Number

[1103522-45-7]

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