Indacaterol Maleate (QAB149)

Alias: QAB149; Indacaterol maleate; QAB-149; QAB 149; trade name: Onbrez Breezhale; arcapta neohaler; Onbrez

Cat No.:V1100 Purity: ≥98%

COA Product Data Instructions for use SDS

Indacaterol Maleate (QAB149) Chemical Structure CAS No.: 753498-25-8
Product category: Adrenergic Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of Indacaterol Maleate (QAB149):

Indacaterol (Onbrez; Arcapta; QAB149)

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

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Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Indacaterol Maleate (formerly known as QAB149; QAB-149; Onbrez Breezhale; arcapta neohaler; Onbrez), the maleate salt of indacaterol, is an approved anti-COPD (chronic obstructive pulmonary disease) drug acting as an ultra-long-acting β-adrenoceptor agonist developed by Novartis. β-adrenoceptor is activated with a pKi of 7.36 in. The FDA approved indacaterol in 2009 to treat chronic obstructive pulmonary disease (COPD). Using a dry powder inhaler, the aerosol formulation is administered. When Chinese hamster ovary cells are transfected with human β2 adrenoceptors and have a pEC50 of 8.06, indacaterol inhibits the production of cAMP.

Biological Activity I Assay Protocols (From Reference)

Targets

β1-adrenoceptor ( pKi = 7.36 ); β2-adrenoceptor ( pKi = 5.48 )

ln Vitro

In vitro activity: Chinese hamster ovary cells transfected with human β2 adrenoceptors show a stable increase in cAMP production in response to indacaterol. With a concentration-dependent mechanism and a pEC50 of 8.23, it prevents electrically induced contraction on the electrically stimulated guinea pig trachea. With a maximum efficacy of 75% in the isolated guinea pig left atrium, indacaterol produces an inotropic effect that is concentration-dependent. Reference [1] The concentration-dependent contraction caused by carbachol is reversed in human small airways by indacaterol, with an IC50 of 37 nM. The serotonin-induced contraction in rat small airways is inversely induced by indacaterol, with an IC50 of 10.5 nM. At 53% in rat small airways and 73% in human small airways, indacaterol has the highest intrinsic efficacy.[2] The effect of indacaterol (10 μM) lasts for 12 hours and causes nearly complete inhibition of the contraction of isolated human bronchi caused by EFS. [3] Indacaterol has an intrinsic activity (Emax of a long-acting indacaterol/Emax of isoprenaline) of 1.03, which means it inhibits the IgE-dependent release of histamine from mast cells. [4] Human airway smooth muscle produces cAMP in response to indacaterol, with a pEC50 of 8.53 and an Emax of 48%. In the primary ASM cells, indacaterol appears to be less effective when compared to the CHO-K1 data. [5]

ln Vivo

In the conscious guinea pig, indacaterol (6.7 μg/kg) has a maximal effect of 85% in inhibiting 5-HT-induced bronchoconstriction. Methacholine-induced bronchoconstriction is dose-dependently inhibited by indacaterol (12.5 μg/kg), with a maximal effect of 85% in the rhesus monkey under anesthesia. [1]

Cell Assay

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.

Animal Protocol

6.7 μg/kg

Guinea pigs

References

[1]. J Pharmacol Exp Ther . 2006 May;317(2):762-70.

[2]. J Pharmacol Exp Ther . 2008 Jan;324(1):270-5.

[3]. Eur Respir J . 2007 Mar;29(3):575-81.

[4]. Br J Pharmacol . 2009 Sep;158(1):267-76.

[5]. Br J Pharmacol . 2009 Sep;158(1):277-86.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C28H32N2O7
Molecular Weight	508.56
Exact Mass	508.22
Elemental Analysis	C, 66.13; H, 6.34; N, 5.51; O, 22.02
CAS #	753498-25-8
Related CAS #	Indacaterol; 312753-06-3
Appearance	Solid powder
SMILES	CCC1=C(C=C2CC(CC2=C1)NC[C@@H](C3=C4C=CC(=O)NC4=C(C=C3)O)O)CC.C(=C\C(=O)O)\C(=O)O
InChi Key	IREJFXIHXRZFER-PCBAQXHCSA-N
InChi Code	InChI=1S/C24H28N2O3.C4H4O4/c1-3-14-9-16-11-18(12-17(16)10-15(14)4-2)25-13-22(28)19-5-7-21(27)24-20(19)6-8-23(29)26-24;5-3(6)1-2-4(7)8/h5-10,18,22,25,27-28H,3-4,11-13H2,1-2H3,(H,26,29);1-2H,(H,5,6)(H,7,8)/b;2-1-/t22-;/m0./s1
Chemical Name	(Z)-but-2-enedioic acid;5-[(1R)-2-[(5,6-diethyl-2,3-dihydro-1H-inden-2-yl)amino]-1-hydroxyethyl]-8-hydroxy-1H-quinolin-2-one
Synonyms	QAB149; Indacaterol maleate; QAB-149; QAB 149; trade name: Onbrez Breezhale; arcapta neohaler; Onbrez
HS Tariff Code	2934.99.9001
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 100~102 mg/mL (196.6~200.6 mM)

Water: <1 mg/mL

Ethanol: <1 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (4.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

Solubility in Formulation 2: ≥ 1.43 mg/mL (2.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 3: ≥ 1.43 mg/mL (2.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

Solubility in Formulation 4: 4% DMSO+30% PEG 300+ddH2O: 10mg/mL

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		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
	10 mM	0.1966 mL	0.9832 mL	1.9663 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06035393	Not yet recruiting	Drug: HRG2005 inhalation Drug: Placebo to match HRG2005 inhalation	Chronic Obstructive Pulmonary Disease	Jiangsu HengRui Medicine Co., Ltd.	October 27, 2023	Phase 2
NCT01377051	Completed	Drug: Indacaterol maleate Drug: Placebo	COPD Dyspnea Hypoxemia	University of Milan	May 2011	Phase 4
NCT01985334	Completed	Drug: Glycopyrronium Drug: SABA Drug: LAMA	COPD	Novartis Pharmaceuticals	February 14, 2014	Phase 4
NCT00556673	Completed	Drug: indacaterol maleate/ mometasone furoate Drug: placebo to indacaterol maleate/ mometasone furoate	Asthma	Novartis	October 2007	Phase 2
NCT00636961	Completed	Drug: Indacaterol 300μg Drug: Placebo	Chronic Obstructive Pulmonary Disease	Novartis	February 2008	Phase 2

Biological Data

Potency and intrinsic efficacy for the compounds in the human (left) and rat (right) small airways contracted to 70% of the maximal closure with carbachol and serotonin, respectively.J Pharmacol Exp Ther.2008 Jan;324(1):270-5.

Indacaterol Maleate — Onset of action for the compounds in the human (left) and rat (right) small airways contracted to 70% of the maximal closure with carbachol and serotonin, respectively.J Pharmacol Exp Ther.2008 Jan;324(1):270-5.

Duration of action for the compounds in the human small airways contracted to 50% of the maximal closure with carbachol.J Pharmacol Exp Ther.2008 Jan;324(1):270-5.