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

Indacaterol maleate  (Synonyms: QAB149)

Cat. No.: HY-14299A Purity: 99.82%
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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.

For research use only. We do not sell to patients.

Indacaterol maleate Chemical Structure

Indacaterol maleate Chemical Structure

CAS No. : 753498-25-8

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Based on 4 publication(s) in Google Scholar

Other Forms of Indacaterol maleate:

Indacaterol maleate Related Antibodies

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Description

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[1][2].

IC50 & Target[1][2]

β adrenergic receptor

 

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].

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

Indacaterol maleate Related Antibodies

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.
In Vivo

Indacaterol maleate (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.
Clinical Trial
Molecular Weight

508.56

Formula

C28H32N2O7
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC2=C(C([C@@H](O)CNC3CC4=C(C=C(CC)C(CC)=C4)C3)=CC=C2O)C=C1.O=C(O)/C=C\C(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (196.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9663 mL 9.8317 mL 19.6634 mL
5 mM 0.3933 mL 1.9663 mL 3.9327 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.09 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.
  • Protocol 2

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

    Solubility: ≥ 1.43 mg/mL (2.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.
Purity & Documentation

Purity: 99.82%

SDS (393 KB)

COA (252 KB) HNMR (279 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9663 mL 9.8317 mL 19.6634 mL 49.1584 mL
5 mM 0.3933 mL 1.9663 mL 3.9327 mL 9.8317 mL
10 mM 0.1966 mL 0.9832 mL 1.9663 mL 4.9158 mL
15 mM 0.1311 mL 0.6554 mL 1.3109 mL 3.2772 mL
20 mM 0.0983 mL 0.4916 mL 0.9832 mL 2.4579 mL
25 mM 0.0787 mL 0.3933 mL 0.7865 mL 1.9663 mL
30 mM 0.0655 mL 0.3277 mL 0.6554 mL 1.6386 mL
40 mM 0.0492 mL 0.2458 mL 0.4916 mL 1.2290 mL
50 mM 0.0393 mL 0.1966 mL 0.3933 mL 0.9832 mL
60 mM 0.0328 mL 0.1639 mL 0.3277 mL 0.8193 mL
80 mM 0.0246 mL 0.1229 mL 0.2458 mL 0.6145 mL
100 mM 0.0197 mL 0.0983 mL 0.1966 mL 0.4916 mL
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Indacaterol maleate Related Classifications

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:

Indacaterol753498-25-8QAB149QAB 149QAB-149Adrenergic ReceptorBeta ReceptorCOPDasthmaHT1080 cellsNF-κBβ-arrestin2myocardial infarctionheart failureInhibitorinhibitorinhibit

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