Macitentan

Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) [1].

Product Specifications

CAS Number

[441798-33-0]

Product Name Alternative

ACT-064992

UNSPSC

12352005

Hazard Statement

H360

Target

Apoptosis; Endothelin Receptor

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease; Endocrinology; Cancer

Assay Protocol

https://www.medchemexpress.com/Macitentan.html

Concentration

10mM

Purity

99.87

Solubility

DMSO : ≥ 50 mg/mL

Smiles

BrC1=CN=C(OCCOC2=C(C3=CC=C(Br)C=C3)C(NS(NCCC)(=O)=O)=NC=N2)N=C1

Molecular Formula

C19H20Br2N6O4S

Molecular Weight

588.27

Precautions

H360

References & Citations

[1]Corallo C, et al. Bosentan and macitentan prevent the endothelial-to-mesenchymal transition (EndoMT) in systemic sclerosis: in vitro study. Arthritis Res Ther. 2016 Oct 6;18 (1) :228.|[2]Sen S, et al. Renal, retinal and cardiac changes in type 2 diabetes are attenuated by macitentan, a dual endothelin receptor antagonist. Life Sci. 2012 Apr 13.|[3]Bruderer S, et al. Effect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissue-targeting dual endothelin receptor antagonist. AAPS J. 2012 Mar;14 (1) :68-78.|[4]Kim SJ, et al. Antivascular therapy for multidrug-resistant ovarian tumors by macitentan, a dual endothelin receptor antagonist. Transl Oncol. 2012 Feb;5 (1) :39-47.