Aprocitentan

CAS No.:1103522-45-7

Aprocitentan is a white to off-white solid powder with a molecular formula of C₁₆H₁₄Br₂N₆O₄S and a molecular weight of approximately 546.19 g/mol. It is highly selective for both ET‑A and ET‑B receptors, with reported IC₅₀ values of 3.4 nM and 987 nM, respectively, for the two receptor subtypes. The compound is soluble in organic solvents such as DMSO and exhibits a plasma half‑life of approximately 44 hours, supporting a convenient once‑daily oral dosing regimen. It is highly bound to plasma proteins, with the powder form typically available in research and pharmaceutical grades (≥98% purity) and recommended to be stored at −20°C (for long‑term stability) or refrigerated at 2‑8°C (for short‑term use), protected from light.

Core Functions:

• Active pharmaceutical ingredient (API) in Tryvio® for the treatment of hypertension in combination with other antihypertensive drugs, specifically to lower blood pressure in adult patients whose hypertension is not adequately controlled on other medications

• Research compound for studying endothelin‑1 pathway regulation, dual ET‑A/ET‑B receptor antagonism, and the pathophysiology of resistant hypertension

• Investigation in specific patient subgroups where the drug has shown enhanced efficacy, including individuals with advanced chronic kidney disease, diabetes, and in Black patients

• Active reference standard for analytical method development and quality control of endothelin receptor antagonists in pharmaceutical testing

• Preclinical and clinical research for evaluating its cardiovascular protective effects, including reduction of albuminuria and other hypertension‑mediated organ damage endpoints