产品
编 号:F449462
分子式:C28H32N2O7
分子量:508.56
产品类型
结构图
CAS No: 753498-25-8
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生物活性:
Indacaterol maleate (QAB149) is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol maleate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used in cardiovascular disease research.
体内研究:
Indacaterol maleate (0.3 mg/kg;口服;每天一次,持续 15 周) 在心力衰竭 (HF) 的心肌梗死 (MI) 大鼠模型中表现出正常化和逆转心脏重塑的活性。Animal Model:Male Wistar rats (225-250 g; myocardial infarction (MI) rat model of heart failure (HF)).
Dosage:0.3 mg/kg
Administration:In animal drinking water; sinle daily for 15 weeks
Result:Significantly reduced both mean arterial blood pressure and heart rate.Increased both systolic and diastolic LVID where in HF, and reversed the decreased ejection fraction (%) values.Significantly reduced the infarct size, and catecholamine values to basal levels.Significantly increased β1 mRNA expression and cardiac cAMP levels in respect to HF.
体外研究:
Indacaterol maleate (1,2.5,5,10 μM;12 h) 抑制人纤维肉瘤 HT1080 细胞中 TNF-α 诱导的 MMP-9 表达和活性。 Indacaterol maleate (10 μM;6 h) 通过降低 MMP-9 的表达和活性来抑制 TNF-α 诱导的人纤维肉瘤细胞的侵袭和迁移。 Indacaterol maleate (1,2.5,5,10 μM;2.5 h) 抑制 HT1080 细胞中 TNF-α 激活的 IKK/NF-кB 信号传导。