Indacaterol maleate (QAB149) 是一种口服有效的超长效ADRB2激动剂。Indacaterol maleate 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 maleate 还可用于心血管疾病的研究。
| 生物活性 | Indacaterol maleate (QAB149) is an orally active ultra-long-actingβ2adrenergic receptor(ADRB2) agonist. Indacaterol maleate inhibitsNF-κBactivity in aβ-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used incardiovascular diseaseresearch[1][2]. |
| IC50& Target[1][2] | |
体外研究
(In Vitro) | Indacaterol maleate (1, 2.5, 5, 10 μM; 12 h) inhibits TNF-α induced MMP-9 expression and activity in human fibrosarcoma HT1080 cells[1].
Indacaterol maleate (10 μM; 6 h) inhibits TNF-α induced invasion and migration of human fibrosarcoma cells by reducing MMP-9 expression and activity[1].
Indacaterol maleate (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. |
|
体内研究
(In Vivo) | Indacaterol maleate (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. |
|
| Clinical Trial | |
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(196.63 mM;Need ultrasonic) H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble) 配制储备液 | 1 mM | 1.9663 mL | 9.8317 mL | 19.6634 mL | | 5 mM | 0.3933 mL | 1.9663 mL | 3.9327 mL | | 10 mM | 0.1966 mL | 0.9832 mL | 1.9663 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.09 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.09 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。 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 1.43 mg/mL (2.81 mM); Clear solution
此方案可获得 ≥ 1.43 mg/mL (2.81 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 14.3 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。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 1.43 mg/mL (2.81 mM); Clear solution
此方案可获得 ≥ 1.43 mg/mL (2.81 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 14.3 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。
|
m.cnreagent.com