Aprocitentan is an orally active, dual endothelin (ET) receptor antagonist developed for the treatment of hypertension in which, despite available treatments, a medical need exists for drugs with a new mechanism of action.
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Name | Aprocitentan |
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Iupac Chemical Name | N-[5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl]sulfuric diamide |
Synonyms | Aprocitentan; ACT-132577; ACT 132577; ACT132577; Despropyl Macitentan. |
Molecular Formula | C16H14Br2N6O4S |
Molecular Weight | 546.19 |
Smile | BrC1=CC=C(C=C1)C=1C(=NC=NC1OCCOC1=NC=C(C=N1)Br)NS(N)(=O)=O |
InChiKey | DKULOVKANLVDEA-UHFFFAOYSA-N |
InChi | InChI=1S/C16H14Br2N6O4S/c17-11-3-1-10(2-4-11)13-14(24-29(19,25)26)22-9-23-15(13)27-5-6-28-16-20-7-12(18)8-21-16/h1-4,7-9H,5-6H2,(H2,19,25,26)(H,22,23,24) |
CAS Number | 1103522-45-7 |
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Formulation | Off-white solid to white solid |
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Purity | 98% Min. |
Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Solubility | Soluble in DMSO, not in water |
Handling | |
Shipping Condition | Shipped under ambient temperature |
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[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