Aprocitentan, CAS 1103522-45-7

Formulation: A solid

Formal Name: N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-sulfamide

Purity: ≥98%

Formula Markup: C16H14Br2N6O4S

Formula Weight: 546,2

Shelf life (days): 1460

CAS Number: 1103522-45-7

Notes: Aprocitentan is a dual endothelin type A (ETA) and ETB receptor antagonist and an active metabolite of macitentan (Item No. 23304).{62420} It is formed from macitentan by the cytochrome P450 (CYP) isoform CYP3A4. Aprocitentan inhibits increases in intracellular calcium induced by endothelin-1 (ET-1) in primary human pulmonary arterial smooth muscle cells (HPASMCs; IC50 = 14 nM), ET-1-induced contractions in isolated rat aortic rings (pA2 = 6.7 for ETA), and sarafotoxin S6c-induced contractions of isolated rat tracheal rings (pKB = 5.5 for ETB).{36210} It reduces ET-1-induced increases in the proliferation of isolated human skin fibroblasts when used at concentrations of 10 and 100 µM.{58774} Aprocitentan (10-300 mg/kg) increases plasma ET-1 concentrations in normotensive rats and decreases mean arterial pressure (MAP) in DOCA-salt hypertensive rats.{58775}

• Artikelnummer: CAY34915-10
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 34915-10
• Green Labware: Nein
• Verpackungseinheit: 10 mg
• Mengeneinheit: STK