2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. Indacaterol

Indacaterol is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol 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 can also be used in cardiovascular disease research.

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Indacaterol

Indacaterol 構造式

CAS 番号 : 312753-06-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 125 在庫あり
Solution
10 mM * 1 mL in DMSO USD 125 在庫あり
Solid
100 mg $114 在庫あり
500 mg $318 在庫あり
1 g   お問い合わせ  
5 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 5 publication(s) in Google Scholar

Other Forms of Indacaterol:

Indacaterol 関連抗体

Top Publications Citing Use of Products

Adrenergic Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
α adrenergic receptor β adrenergic receptor

  • 生物活性

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製品説明

Indacaterol is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol 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 can also be used in cardiovascular disease research[1][2].

IC50 & Target[1][2]

β adrenergic receptor

 

Cellular Effect
Cell Line Type Value Description References
A-431 EC50
1.5 nM
Compound: Indacaterol
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
[PMID: 25065493]
CHO EC50
>1.0 x 10-5M
Compound: Indacaterol
Activity at human D2R expressed in CHO cells by radiolabelled [35S]GTPgammaS assay
Activity at human D2R expressed in CHO cells by radiolabelled [35S]GTPgammaS assay
[PMID: 25065493]
体外実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Indacaterol 関連抗体

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.
体内実験

Indacaterol (0.3 mg/kg; po; 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
分子量

392.49

分子式

C24H28N2O3
CAS 番号
Appearance

Solid

Color

White to yellow

SMILES

OC1=CC=C([C@@H](O)CNC2CC(C=C(CC)C(CC)=C3)=C3C2)C4=C1NC(C=C4)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 62.5 mg/mL (159.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

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体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (5.30 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.98%

COA (251 KB) HNMR (209 KB) LCMS (117 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5478 mL 12.7392 mL 25.4784 mL 63.6959 mL
5 mM 0.5096 mL 2.5478 mL 5.0957 mL 12.7392 mL
10 mM 0.2548 mL 1.2739 mL 2.5478 mL 6.3696 mL
15 mM 0.1699 mL 0.8493 mL 1.6986 mL 4.2464 mL
20 mM 0.1274 mL 0.6370 mL 1.2739 mL 3.1848 mL
25 mM 0.1019 mL 0.5096 mL 1.0191 mL 2.5478 mL
30 mM 0.0849 mL 0.4246 mL 0.8493 mL 2.1232 mL
40 mM 0.0637 mL 0.3185 mL 0.6370 mL 1.5924 mL
50 mM 0.0510 mL 0.2548 mL 0.5096 mL 1.2739 mL
60 mM 0.0425 mL 0.2123 mL 0.4246 mL 1.0616 mL
80 mM 0.0318 mL 0.1592 mL 0.3185 mL 0.7962 mL
100 mM 0.0255 mL 0.1274 mL 0.2548 mL 0.6370 mL
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Indacaterol Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Indacaterol312753-06-3Adrenergic ReceptorBeta ReceptorCOPDasthmaHT1080 cellsNF-κBβ-arrestin2myocardial infarctionheart failureInhibitorinhibitorinhibit

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製品番号:
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