Formulation: A solid
Formal Name: N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy-1,1,2,2-d4]-4-pyrimidinyl]-N'-propyl-sulfamide
Purity: ≥99% deuterated forms (d1-d4)
Formula Markup: C19H16Br2D4N6O4S
Formula Weight: 592,3
Shelf life (days): 730
CAS Number: 1258428-05-5
Notes: Macitentan-d4 is intended for use as an internal standard for the quantification of macitentan (Item No. 23304) by GC- or LC-MS. Macitentan is a dual antagonist of the endothelin (ET) receptors type A and B (IC50s = 0.5 and 391 nM in a radioligand binding assay using recombinant ETA and ETB, respectively).{36210} Macitentan inhibits intracellular Ca2+ increases induced by the endothelin isoform ET-1 in human pulmonary arterial smooth muscle cells (HPASMCs; IC50 = 0.9 nM), contractions of isolated rat aortic rings (pA2 = 7.6 for ETA), and sarafotoxin S6c-induced contractions of isolated rat tracheal rings (pA2 = 5.9 for ETB). Macitentan increases plasma ET-1 concentrations in normotensive rats and decreases mean arterial blood pressure in DOCA-salt hypertensive rats (ED50 = 1 mg/kg). Oral administration (30 mg/kg per day) prevents development of pulmonary hypertension and right ventricle hypertrophy in a rat model of hypertension induced by monocrotaline (Item No. 16666). It also decreases the number of vascular and tubule-interstitial lesions and amount of glomerular damage in a rat model of diabetes induced by streptozotocin (Item No. 13104). Formulations containing macitentan have been used for the treatment of pulmonary arterial hypertension.{36211}
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