Indacaterol 是一种口服有效的超长效ADRB2激动剂。Indacaterol 能以β-arrestin2依赖的方式抑制NF-κB活性,防止进一步的肺部损伤,并改善慢性阻塞性肺病 (COPD) 的肺功能。Indacaterol 还可用于心血管疾病的研究。
生物活性 | Indacaterol is an orally active ultra-long-actingβ2adrenergic receptor(ADRB2) agonist. Indacaterol inhibitsNF-κBactivity in aβ-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol can also be used incardiovascular diseaseresearch[1][2]. |
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体外研究 (In Vitro) | Indacaterol (1, 2.5, 5, 10 μM; 12 h) inhibits TNF-α induced MMP-9 expression and activity in human fibrosarcoma HT1080 cells[1]. Indacaterol (10 μM; 6 h) inhibits TNF-α induced invasion and migration of human fibrosarcoma cells by reducing MMP-9 expression and activity[1]. Indacaterol (1, 2.5, 5, 10 μM; 2.5 h) inhibits TNF-α-activated IKK/NF-кB signaling in HT1080 cells[1].
Cell Viability Assay[1] Cell Line: | HT1080 cells (constitutively express MMP-9) | Concentration: | 1, 2.5, 5, 10 μM | Incubation Time: | 12 h (pretreat) | Result: | Significantly suppressed MMP-9 mRNA expression in the 2.5 to 10 μM range. |
Cell Migration Assay[1] Cell Line: | HT1080 cells (constitutively express MMP-9) | Concentration: | 10 μM | Incubation Time: | 6 h (pretreat for 2 h, then incubat with TNF-α for 4 h) | Result: | Significantly reduced cell migration of fibrosarcoma and inhibited HT1080 cell migration in the zone of wound healing. |
Western Blot Analysis[1] Cell Line: | HT1080 cells | Concentration: | 1, 2.5, 5, 10 μM | Incubation Time: | 2.5 h (pretreat for 2 h, then incubat with TNF-α for 0.5 h) | Result: | Suppressed TNF-α induced the phosphorylation of IκBα and IKKα/β (the upstream activators of NF-κB). Inhibited TNF-α-induced NF-κB nuclear translocation when at 5 and 10 μM. Suppressed TNF-α-induced MMP-9 enzyme activity and decreased MMP-9 protein levels in a dose-dependent manner in the 2.5 to 10 μM range. |
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体内研究 (In Vivo) | Indacaterol (0.3 mg/kg; in animal drinking water; sinle daily for 15 weeks) shows activity of normalizing and reversing cardiac remodeling in a myocardial infarction (MI) rat model of heart failure (HF)[2].
Animal Model: | Male Wistar rats (225-250 g; myocardial infarction (MI) rat model of heart failure (HF))[2]. | 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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 62.5 mg/mL(159.24 mM;Need ultrasonic) 配制储备液 1 mM | 2.5478 mL | 12.7392 mL | 25.4784 mL | 5 mM | 0.5096 mL | 2.5478 mL | 5.0957 mL | 10 mM | 0.2548 mL | 1.2739 mL | 2.5478 mL |
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此方案可获得 ≥ 2.08 mg/mL (5.30 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.30 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.30 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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