您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Indacaterol
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Indacaterol
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Indacaterol图片
CAS NO:312753-06-3
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
100mg电议
500mg电议
1 g电议
5 g电议

产品名称
茚达特罗
产品介绍
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].

IC50& Target[1][2]

β-adrenoceptor

 

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.
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.
Clinical Trial
分子量

392.49

性状

Solid

Formula

C24H28N2O3

CAS 号

312753-06-3

中文名称

茚达特罗

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 62.5 mg/mL(159.24 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5478 mL12.7392 mL25.4784 mL
5 mM0.5096 mL2.5478 mL5.0957 mL
10 mM0.2548 mL1.2739 mL2.5478 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。-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    40%PEG300   5%Tween-80   45% 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 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 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。