Aprocitentan

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Aprocitentan

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Cat No: 34915

Biochemicals - Receptor Pharmacology

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 int...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

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

Correlated keywords:

ACT132577

Product Overview:
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}

Size	1 mg
Shipping	dry ice
CAS Number	1103522-45-7
Molecular Formula	C₁₆H₁₄Br₂N₆O₄S
SMILES	O=S(N)(NC1=NC=NC(OCCOC2=NC=C(C=N2)Br)=C1C3=CC=C(C=C3)Br)=O
Molecular Weight	546,2
Formulation	A solid
Purity	≥98%
Custom Code	2933.59
UNSPSC code	12352100

Technical File

MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.