Macitentan - CAS 441798-33-0
Catalog number: B0084-092460
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
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Targets:
Endothelin Receptor
Description:
Macitentan is an orally available dual endothelin receptor (ETR) antagonist with potential antihypertensive and antineoplastic activity.
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Catalog Number Size Price Stock Quantity
B0084-092460 1 g $399 In stock
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Synonyms:
ACT-064992; ACT064992; ACT 064992
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Current Developer:
Actelion
1.Treatment of idiopathic pulmonary fibrosis: a network meta-analysis.
Rochwerg B1,2,3, Neupane B4, Zhang Y5,6, Garcia CC7,8,9, Raghu G10, Richeldi L11, Brozek J12,13, Beyene J14, Schünemann H15,16,17. BMC Med. 2016 Feb 3;14(1):18. doi: 10.1186/s12916-016-0558-x.
BACKGROUND: Idiopathic pulmonary fibrosis (IPF) is an interstitial lung disease associated with high morbidity and mortality. Effective treatments for IPF are limited. Several recent studies have investigated novel therapeutic agents for IPF, but very few have addressed their comparative benefits and harms.
2.Endothelin.
Davenport AP1, Hyndman KA2, Dhaun N2, Southan C2, Kohan DE2, Pollock JS2, Pollock DM2, Webb DJ2, Maguire JJ2. Pharmacol Rev. 2016 Apr;68(2):357-418. doi: 10.1124/pr.115.011833.
The endothelins comprise three structurally similar 21-amino acid peptides. Endothelin-1 and -2 activate two G-protein coupled receptors, ETA and ETB, with equal affinity, whereas endothelin-3 has a lower affinity for the ETA subtype. Genes encoding the peptides are present only among vertebrates. The ligand-receptor signaling pathway is a vertebrate innovation and may reflect the evolution of endothelin-1 as the most potent vasoconstrictor in the human cardiovascular system with remarkably long lasting action. Highly selective peptide ETA and ETB antagonists and ETB agonists together with radiolabeled analogs have accurately delineated endothelin pharmacology in humans and animal models, although surprisingly no ETA agonist has been discovered. ET antagonists (bosentan, ambrisentan) have revolutionized the treatment of pulmonary arterial hypertension, with the next generation of antagonists exhibiting improved efficacy (macitentan). Clinical trials continue to explore new applications, particularly in renal failure and for reducing proteinuria in diabetic nephropathy.
3.Endothelin receptor antagonist macitentan or deletion of mouse mast cell protease 4 delays lesion development in atherosclerotic mice.
Houde M1, Desbiens L1, Schwertani A2, Pejler G3, Iglarz M4, D'Orléans-Juste P5. Life Sci. 2016 Mar 12. pii: S0024-3205(16)30169-2. doi: 10.1016/j.lfs.2016.03.018. [Epub ahead of print]
AIMS: To determine the impact of mixed endothelin receptor antagonist and mouse mast cell protease-4 (mMCP-4) in the development of atherosclerosis in the mouse model.
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CAS 441798-33-0 Macitentan

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