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| 100mg |
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| 250mg |
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Purity: ≥98%
Indacaterol (formerly known as QAB-149) is an anti-COPD drug acting as an ultra-long-acting β-adrenoceptor agonist developed by Novartis with pKi of 7.36. In order to treat chronic obstructive pulmonary disease (COPD), the FDA approved indacaterol in 2009. With the use of a dry powder inhaler, it is administered as an aerosol. Chinese hamster ovary cells transfected with human β2 adrenoceptors stably exhibit a pEC50 of 8.06, indicating that indacaterol inhibits the production of cAMP.
| Targets |
β1-adrenoceptor ( pKi = 7.36 ); β2-adrenoceptor ( pKi = 5.48 )
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|---|---|
| ln Vitro |
Indacaterol (1, 2.5, 5, 10 μM; 12 h) inhibits TNF-α-induced MMP-9 and expression activity in human fibrosarcoma HT1080 cells [1]. Indacaterol (10 μM; 6 h) reduces the expression activity of MMP-9 [1]. Indacaterol (1, 2.5, 5, 10 μM; 2.5 h) inhibits TNF-α-activated IKK/NF-кB expression and activity in HT1080 cells and inhibits TNF-α-activated human fibrosarcoma cells most effectively and migrates [ 1]. Cell Viability Assay[1] Cell Line: HT1080 cells (constitutivelyexpress MMP-9) Concentration: 1, 2.5, 5, 10 µM Incubation Time: 12 h (pretreat) Results: Significantly inhibited MMP-9 mRNA. Expression range is 2.5 to 10 µM. Cell migration assay[1] Cell line: HT1080 cells (constitutively expressing MMP-9) Concentration: 10 µM Incubation time: 6 hours (2 hours pretreatment followed by 4 hours incubation with TNF-α) Results: Significant reduction of fibrosarcoma and inhibited HT1080 cell migration in the wound healing area. Western Blot Analysis[1] Cell line: HT1080 Cell concentration: 1, 2.5, 5, 10 µM Incubation time: 2.5 hours (pretreatment for 2 hours, then incubated with TNF-α for 0.5 hours) Results: Inhibition of TNF-α induction of IκBα and Phosphorylation of IKKα/β, the upstream activator of NF-κB. Inhibits TNF-α-induced NF-κB nuclear translocation at 5 and 10 µM. Inhibits TNF-α-induced MMP-9 enzyme activity and reduces MMP-9 protein levels in a dose-dependent manner in the range of 2.5 to 10 µM.
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| ln Vivo |
Indacaterol (0.3 mg/kg; MI; once daily for 15 weeks) exhibits normalizing and MI-restoring activity in a myocardial infarction (MI) cardiovascular model of heart failure (HF) [2]. Male Wistar rats (225-250 g; heart failure (HF) myocardial infarction (MI) rat model) [2]. Dosage: 0.3 mg/kg Administration: In drinking water of animals; once daily for 15 weeks Results: Mean arterial blood pressure and heart rate were significantly reduced. Both systolic and diastolic blood pressure LVID increase in heart failure and reverse the decrease in ejection fraction (%) values. Significantly reduced infarct size and catecholamine values to basal levels. β1 mRNA expression and cardiac cAMP levels were significantly increased in association with HF.
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| 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 |
Male Wistar rats (225-250 g; myocardial infarction (MI) rat model of heart failure (HF))
0.3 mg/kg In animal drinking water; sinle daily for 15 weeks |
| References |
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| Molecular Formula |
C24H28N2O3
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|---|---|
| Molecular Weight |
392.49100
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| Exact Mass |
392.21
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| Elemental Analysis |
C, 73.44; H, 7.19; N, 7.14; O, 12.23
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| CAS # |
312753-06-3
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| Related CAS # |
Indacaterol maleate; 753498-25-8; Indacaterol-d3; 2699828-16-3
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| Appearance |
Solid powder
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| SMILES |
CCC1=C(C=C2CC(CC2=C1)NC[C@@H](C3=C4C=CC(=O)NC4=C(C=C3)O)O)CC
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| InChi Key |
QZZUEBNBZAPZLX-QFIPXVFZSA-N
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| InChi Code |
InChI=1S/C24H28N2O3/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/h5-10,18,22,25,27-28H,3-4,11-13H2,1-2H3,(H,26,29)/t22-/m0/s1
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| Chemical Name |
5-[(1R)-2-[(5,6-diethyl-2,3-dihydro-1H-inden-2-yl)amino]-1-hydroxyethyl]-8-hydroxy-1H-quinolin-2-one
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| Synonyms |
QAB-149; QAB149; QAB149; QAB149-AFA; QAB-149-AFA; Arcapta; Onbrez
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: 52~62.5 mg/mL (132.5~159.2 mM)
Ethanol: ~20 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.30 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 20.8 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.30 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*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.
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.
(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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06067100 | Recruiting | Drug: Placebo Drug: Indacaterol and Mometasonefluroate (low dose) |
Exercise Performance | Morten Hostrup, PhD | October 5, 2023 | Not Applicable |
| NCT05562466 | Recruiting | Drug: QMF149 Drug: Budesonide |
Asthma | Novartis Pharmaceuticals | May 11, 2023 | Phase 3 |
| NCT06077019 | Recruiting | Drug: Placebo Drug: Vilanterol and Fluticasone Furoate |
Exercise Performance | Morten Hostrup, PhD | October 5, 2023 | Not Applicable |
| NCT05776927 | Not yet recruiting | Drug: QVM149 Device: Girohaler |
Asthma | Novartis Pharmaceuticals | December 23, 2024 | Phase 3 |
| NCT06035393 | Not yet recruiting | Drug: HRG2005 inhalation Drug: Placebo to match HRG2005n inhalation |
Chronic Obstructive Pulmonary Disease |
Jiangsu HengRui Medicine Co., Ltd. |
October 27, 2023 | Phase 2 |
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