WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 319521
CAS#: 753498-25-8 (malate)
Description: Indacaterol is an ultra-long-acting beta-adrenoceptor agonist developed by Novartis. It was approved in 2009. It is licensed only for the treatment of chronic obstructive pulmonary disease (COPD) (long-term data in patients with asthma are thus far lacking). It is delivered as an aerosol formulation through a dry powder inhaler.
MedKoo Cat#: 319521
Name: Indacaterol maleate
CAS#: 753498-25-8 (malate)
Chemical Formula: C28H32N2O7
Exact Mass:
Molecular Weight: 508.571
Elemental Analysis: C, 66.13; H, 6.34; N, 5.51; O, 22.02
Related CAS #: 753498-25-8 (malate) 312753-06-3 (free base)
Synonym: QAB-149; QAB 149; QAB149; Indacaterol maleate; trade name Onbrez Breezhale; arcapta neohaler; Onbrez.
IUPAC/Chemical Name: (R)-5-(2-((5,6-diethyl-2,3-dihydro-1H-inden-2-yl)amino)-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one maleate
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
SMILES Code: 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
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 508.571 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
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2: Horita N, Kaneko T. Role of combined indacaterol and glycopyrronium bromide (QVA149) for the treatment of COPD in Japan. Int J Chron Obstruct Pulmon Dis. 2015 Apr 21;10:813-22. doi: 10.2147/COPD.S56067. eCollection 2015. Review. PubMed PMID: 25960646; PubMed Central PMCID: PMC4410821.
3: Matera MG, Rogliani P, Cazzola M. QVA149 (indacaterol/glycopyrronium) for the treatment of chronic obstructive pulmonary disease. Expert Opin Pharmacother. 2015 May;16(7):1079-90. doi: 10.1517/14656566.2015.1032247. Epub 2015 Apr 5. Review. PubMed PMID: 25843089.
4: Pelaia G, Maselli R, Gallelli L. Pharmacologic rationale, efficacy and safety of the fixed-dose co-formulation of indacaterol and glycopyrronium. Multidiscip Respir Med. 2014 Dec 8;9(1):64. doi: 10.1186/2049-6958-9-64. eCollection 2014. Review. PubMed PMID: 25699181; PubMed Central PMCID: PMC4333835.
5: Ridolo E, Montagni M, Riario-Sforza GG, Baroni M, Incorvaia C. Combination therapy with indacaterol and glycopyrronium bromide in the management of COPD: an update on the evidence for efficacy and safety. Ther Adv Respir Dis. 2015 Apr;9(2):49-55. doi: 10.1177/1753465815572065. Epub 2015 Feb 17. Review. PubMed PMID: 25691493.
6: Prakash A, Babu KS, Morjaria JB. Profile of inhaled glycopyrronium bromide as monotherapy and in fixed-dose combination with indacaterol maleate for the treatment of COPD. Int J Chron Obstruct Pulmon Dis. 2015 Jan 7;10:111-23. doi: 10.2147/COPD.S67758. eCollection 2015. Review. PubMed PMID: 25609944; PubMed Central PMCID: PMC4293295.
7: Pelaia G, Maselli R, Matera MG. Treatment of chronic obstructive pulmonary disease by dual bronchodilation with coformulation of indacaterol/glycopyrronium. Pharmacology. 2014;94(5-6):249-58. doi: 10.1159/000368986. Epub 2014 Nov 28. Review. PubMed PMID: 25471458.
8: Murphy L, Rennard S, Donohue J, Molimard M, Dahl R, Beeh KM, Dederichs J, Fülle HJ, Higgins M, Young D. Turning a molecule into a medicine: the development of indacaterol as a novel once-daily bronchodilator treatment for patients with COPD. Drugs. 2014 Sep;74(14):1635-57. doi: 10.1007/s40265-014-0284-7. Review. PubMed PMID: 25212789.
9: Roskell NS, Anzueto A, Hamilton A, Disse B, Becker K. Once-daily long-acting beta-agonists for chronic obstructive pulmonary disease: an indirect comparison of olodaterol and indacaterol. Int J Chron Obstruct Pulmon Dis. 2014 Jul 31;9:813-24. doi: 10.2147/COPD.S59673. eCollection 2014. Review. PubMed PMID: 25114521; PubMed Central PMCID: PMC4124050.
10: Ulrik CS. Clinical benefit of fixed-dose dual bronchodilation with glycopyrronium and indacaterol once daily in patients with chronic obstructive pulmonary disease: a systematic review. Int J Chron Obstruct Pulmon Dis. 2014 Apr 1;9:331-8. doi: 10.2147/COPD.S60362. eCollection 2014. Review. PubMed PMID: 24729699; PubMed Central PMCID: PMC3979690.
11: Frampton JE. QVA149 (indacaterol/glycopyrronium fixed-dose combination): a review of its use in patients with chronic obstructive pulmonary disease. Drugs. 2014 Mar;74(4):465-88. doi: 10.1007/s40265-014-0194-8. Review. PubMed PMID: 24604791.
12: Rodrigo GJ, Plaza V. Efficacy and safety of a fixed-dose combination of indacaterol and Glycopyrronium for the treatment of COPD: a systematic review. Chest. 2014 Aug;146(2):309-17. doi: 10.1378/chest.13-2807. Review. PubMed PMID: 24556877.
13: Seth HD, Sultan S, Gotfried MH. Role of indacaterol, a once-daily bronchodilator, in chronic obstructive pulmonary disease. J Thorac Dis. 2013 Dec;5(6):806-14. doi: 10.3978/j.issn.2072-1439.2013.10.11. Review. PubMed PMID: 24409359; PubMed Central PMCID: PMC3886694.
14: Steiropoulos P, Archontogeorgis K, Nena E, Bouros D. New developments in the management of COPD: clinical utility of indacaterol 75 μg. Int J Chron Obstruct Pulmon Dis. 2014;9:1-7. doi: 10.2147/COPD.S24940. Epub 2013 Dec 6. Review. PubMed PMID: 24353414; PubMed Central PMCID: PMC3862584.
15: Cazzola M, Calzetta L, Page CP, Matera MG. Use of indacaterol for the treatment of COPD: a pharmacokinetic evaluation. Expert Opin Drug Metab Toxicol. 2014 Jan;10(1):129-37. doi: 10.1517/17425255.2014.865723. Epub 2013 Dec 3. Review. PubMed PMID: 24295085.
16: Ridolo E, Montagni M, Olivieri E, Riario-Sforza GG, Incorvaia C. Role of indacaterol and the newer very long-acting β2-agonists in patients with stable COPD: a review. Int J Chron Obstruct Pulmon Dis. 2013;8:425-32. doi: 10.2147/COPD.S49179. Epub 2013 Sep 18. Review. PubMed PMID: 24082783; PubMed Central PMCID: PMC3785397.
17: Chung VC, Ma PH, Hui DS, Tam WW, Tang JL. Indacaterol for chronic obstructive pulmonary disease: systematic review and meta-analysis. PLoS One. 2013 Aug 14;8(8):e70784. doi: 10.1371/journal.pone.0070784. eCollection 2013. Review. PubMed PMID: 23967106; PubMed Central PMCID: PMC3743831.
18: Rossi A, Polese G. Indacaterol: a comprehensive review. Int J Chron Obstruct Pulmon Dis. 2013;8:353-63. doi: 10.2147/COPD.S21625. Epub 2013 Jul 25. Review. PubMed PMID: 23922496; PubMed Central PMCID: PMC3728154.
19: Schachter EN. Indacaterol/glycopyrronium bromide fixed-dose combination for the treatment of COPD. Drugs Today (Barc). 2013 Jul;49(7):437-46. doi: 10.1358/dot.2013.49.7.1980496. Review. PubMed PMID: 23914352.
20: Han J, Dai L, Zhong N. Indacaterol on dyspnea in chronic obstructive pulmonary disease: a systematic review and meta-analysis of randomized placebo-controlled trials. BMC Pulm Med. 2013 Apr 25;13:26. doi: 10.1186/1471-2466-13-26. Review. PubMed PMID: 23617268; PubMed Central PMCID: PMC3651265.
