CAS No. : 1103522-45-7

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000425
Molecular Formula:C16H14Br2N6O4S
Molecular Weight:546.19
Target:endothelin receptor antagonist
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Appearance:Solid powder
Purity: > 98%
Cat No:I000425
Cas No:1103522-45-7

ACT-132577 is the major and pharmacologically active metabolite of macitentan(ACT-064992), which is dual ETA/ETB endothelin (ET) receptor antagonist designed for tissue targeting.
IC50 value:
Tareget: ETA/ETA receptor
In vivo, macitentan is metabolized into a major and pharmacologically active metabolite, ACT-132577. Macitentan and its metabolite antagonized the specific binding of ET-1 on membranes of cells overexpressing ET(A) and ET(B) receptors and blunted ET-1-induced calcium mobilization in various natural cell lines, with inhibitory constants within the nanomolar range. In functional assays, macitentan and ACT-132577 inhibited ET-1-induced contractions in isolated endothelium-denuded rat aorta (ET(A) receptors) and sarafotoxin S6c-induced contractions in isolated rat trachea (ET(B) receptors). In rats with pulmonary hypertension, macitentan prevented both the increase of pulmonary pressure and the right ventricle hypertrophy, and it markedly improved survival [1]. In both ethnic groups, females had an approximately 15% higher exposure to ACT-132577 than male subjects [2]. ACT-132577, a metabolite with lower potency than macitentan, had a half-life of about 48hours and accumulated approximately 8.5-fold [3].

1:Int J Clin Exp Med. 2015 Oct 15;8(10):18420-6. eCollection 2015. Pharmacokinetic study of ACT-132577 in rat plasma by ultra performance liquid chromatography-tandem mass spectrometry.Zhang J,Geng P,Luo X,Zhou G,Lin Y,Zhang L,Wang S,Wen C,Ma J,Ding T, PMID: 26770447 PMCID: PMC4694347
Abstract: It was reported that macitentan was metabolized predominantly by cytochrome P450 3A4, and ACT-132577, its pharmacologically active metabolite, is fivefold less potent at blocking ET receptors than macitentan. In this work, a sensitive and selective ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for determination of ACT-132577 in rat plasma was developed and validated. After addition of diazepam as an internal standard (IS), protein precipitation by acetonitrile was used to prepare samples. Chromatographic separation was achieved on a UPLC BEH C18 column (2.1 mm × 100 mm, 1.7 μm) with 0.2% formic acid and methanol as the mobile phase with gradient elution. An electrospray ionization source was applied and operated in positive ion mode; multiple reactions monitoring (MRM) mode was used for quantification using target fragment ions m/z 546.9→200.6 for ACT-132577, and m/z 285.1→193.1 for IS. Calibration plots were linear throughout the range 10-4000 ng/mL for ACT-132577 in rat plasma. Mean recovery of ACT-132577 in rat plasma ranged from 82.6% to 90.6%, matrix effect of ACT-132577 in rat plasma ranged from 101.4% to 115.2%. RSD of intra-day and inter-day precision were both less than 11%. The accuracy of the method ranged from 96.1% to 103.5%. The method was successfully applied to pharmacokinetic study of ACT-132577 after oral and intravenous administration of macitentan.
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