| Name | Macitentan |
| Description | Macitentan (ACT-064992) is an endothelin receptor antagonist utilized in the treatment of pulmonary arterial hypertension (PAH). |
| In vitro | In DOCA-salt-induced hypertensive rats, Macitentan (10 mg/kg) demonstrated a dose-dependent reduction in mean arterial blood pressure. Similarly, in a model of pulmonary arterial hypertension using monocrotaline-treated rats, oral administration of Macitentan (30 mg/kg/day) dose-dependently prevented the development of pulmonary arterial hypertension and right ventricular hypertrophy. Additionally, in type 2 diabetic db/db mice, oral Macitentan (25 mg/kg/day) reduced mRNA expression while concurrently enhancing NF-κB activation. |
| In vivo | In primary human lung smooth muscle cells (IC50=1 nM), Macitentan inhibits the increase of intracellular calcium ions induced by ET-1. Additionally, Macitentan suppresses ET-1-induced contraction in isolated rat aortic rings. Furthermore, in isolated rat tracheal rings, Macitentan inhibits contraction induced by S6c. |
| Storage | store at low temperature,keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (158.09 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (5.61 mM), Sonication is recommended.
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| Keywords | pulmonary | orally | non-peptide | Macitentan | Inhibitor | inhibit | idiopathic | hypertension | fibrosis | ET-B | ETB | ET-A | ETA | EndothelinReceptor | Endothelin Receptor | endothelin | arterial | Apoptosis | ACT064992 | ACT 064992 |
| Inhibitors Related | Stavudine | Aceglutamide | Tamoxifen | Urea | Cysteamine hydrochloride | Gum arabic | Sodium 4-phenylbutyrate | Metronidazole | Citric Acid Triammonium | Dimethyl phthalate | Alginic acid | Dextran sulfate sodium salt (MW 5000) |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
