A dual ETA/ETB receptor antagonist (IC50s = 0.5 and 391 nM in a radioligand binding assay using recombinant ETA and ETB

Macitentan – 100 mg

Brand:
Cayman
CAS:
441798-33-0
Storage:
-20
UN-No:
Non-Hazardous - /

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 hypertensive DOCA-salt 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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Description

A dual ETA/ETB receptor antagonist (IC50s = 0.5 and 391 nM in a radioligand binding assay using recombinant ETA and ETB, respectively); inhibits ET-1-induced intracellular Ca2+ increase in HPASMCs (IC50 = 0.9 nM) and 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); decreases mean arterial blood pressure in hypertensive DOCA-salt rats (ED50 = 1 mg/kg); prevents development of pulmonary hypertension and right ventricle hypertrophy in a rat model of hypertension; decreases the number of vascular and tubule-interstitial lesions and amount of glomerular damage in a rat model of diabetes

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

Synonyms:  ACT-064992

Molecular weight: 588.3

CAS: 441798-33-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Heart|Myocardial Hypertrophy||Research Area|Cardiovascular System|Kidney & Renal Disease||Research Area|Cardiovascular System|Vasculature|Endothelium||Research Area|Cardiovascular System|Vasculature|Smooth Muscle Cells||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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