Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Macitentan (ACT-064992) is an endothelin receptor antagonist that is used in the therapy of pulmonary arterial hypertension (PAH).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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5 mg | 在庫あり | ¥ 10,000 | |||
10 mg | 在庫あり | ¥ 14,000 | |||
50 mg | 在庫あり | ¥ 19,500 | |||
100 mg | 在庫あり | ¥ 29,000 | |||
500 mg | 在庫あり | ¥ 68,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 13,000 |
説明 | Macitentan (ACT-064992) is an endothelin receptor antagonist that is used in the therapy of pulmonary arterial hypertension (PAH). |
ターゲット&IC50 | ETB:391 nM, ETA:0.5 nM |
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. |
別名 | ACT-064992 |
分子量 | 588.27 |
分子式 | C19H20Br2N6O4S |
CAS No. | 441798-33-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 93 mg/mL (158.1 mM)
You can also refer to dose conversion for different animals. 詳細
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Macitentan 441798-33-0 Apoptosis GPCR/G Protein Endothelin Receptor endothelin non-peptide arterial pulmonary idiopathic Inhibitor ETB orally inhibit ACT064992 fibrosis hypertension ACT-064992 ETA ACT 064992 inhibitor