MedKoo Cat#: 314224 | Name: Indacaterol
Featured

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Indacaterol is an ultra-long-acting beta-adrenoceptor agonist developed by Novartis. It was approved by the European Medicines Agency (EMA) under the trade name Onbrez on November 30, 2009, and by the United States Food and Drug Administration (FDA), under the trade name Arcapta Neohaler, on July 1, 2011. It needs to be taken only once a day, unlike the related drugs formoterol and salmeterol. 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. (Source: http://en.wikipedia.org/wiki/Indacaterol).

Chemical Structure

Indacaterol
Indacaterol
CAS#312753-06-3 (free base)

Theoretical Analysis

MedKoo Cat#: 314224

Name: Indacaterol

CAS#: 312753-06-3 (free base)

Chemical Formula: C24H28N2O3

Exact Mass: 392.2100

Molecular Weight: 392.50

Elemental Analysis: C, 73.44; H, 7.19; N, 7.14; O, 12.23

Price and Availability

Size Price Availability Quantity
100mg USD 450.00 2 Weeks
200mg USD 750.00 2 Weeks
500mg USD 1,250.00 2 Weeks
Bulk Inquiry
Buy Now
Add to Cart
Synonym
Arcapta; 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
InChi Key
QZZUEBNBZAPZLX-QFIPXVFZSA-N
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
SMILES Code
O=C1NC2=C(C([C@@H](O)CNC3CC4=C(C=C(CC)C(CC)=C4)C3)=CC=C2O)C=C1
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.
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
More Info
Product Data
Biological target:
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.
In vitro activity:
As shown in Fig. 2A, TNF-α induced the phosphorylation of IκBα and IKKα/β (the upstream activators of NF-κB), but indacaterol pretreatments (both 5 and 10 μM) under the same conditions suppressed their phosphorylation. Moreover, consistent with this result, TNF-α-induced NF-κB nuclear translocation was also largely inhibited by pretreatments with 5 and 10 μM indacaterol (Fig. 2B). Therefore, these results suggest that indacaterol may inhibit NF-κB-dependent target gene expression by reducing the activity of NF-κB upstream activators. Reference: Mol Cells. 2014 Aug;37(8):585-91. https://pubmed.ncbi.nlm.nih.gov/25134539/
In vivo activity:
Treatment with either metoprolol or indacaterol alone significantly reduced the infarct size (8.50 ± 0.87% and 12.50 ± 1.44%, respectively; P < 0.001) with respect to untreated animals. Metoprolol or indacaterol alone or in combination significantly reduced cardiac GRK2 expression after 15 weeks in the failing rat hearts (Figure 2D, E). Reference: Br J Pharmacol. 2015 Jul;172(14):3627-37. https://pubmed.ncbi.nlm.nih.gov/25825265/
Solvent mg/mL mM
Solubility
DMF:PBS (pH 7.2) (1:3) 0.3 0.64
DMSO 43.2 109.98
Ethanol 10.5 26.75
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 392.50 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.

Recalculate based on batch purity %
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
Formulation protocol:
1. Lee SU, Ahn KS, Sung MH, Park JW, Ryu HW, Lee HJ, Hong ST, Oh SR. Indacaterol inhibits tumor cell invasiveness and MMP-9 expression by suppressing IKK/NF-κB activation. Mol Cells. 2014 Aug;37(8):585-91. doi: 10.14348/molcells.2014.0076. Epub 2014 Aug 18. PMID: 25134539; PMCID: PMC4145369. 2. Scola AM, Loxham M, Charlton SJ, Peachell PT. The long-acting beta-adrenoceptor agonist, indacaterol, inhibits IgE-dependent responses of human lung mast cells. Br J Pharmacol. 2009 Sep;158(1):267-76. doi: 10.1111/j.1476-5381.2009.00178.x. Epub 2009 Apr 9. PMID: 19371332; PMCID: PMC2795262. 3. Rinaldi B, Donniacuo M, Sodano L, Gritti G, Martuscelli E, Orlandi A, Rafaniello C, Rossi F, Calzetta L, Capuano A, Matera MG. Effects of chronic treatment with the new ultra-long-acting β2 -adrenoceptor agonist indacaterol alone or in combination with the β1 -adrenoceptor blocker metoprolol on cardiac remodelling. Br J Pharmacol. 2015 Jul;172(14):3627-37. doi: 10.1111/bph.13148. Epub 2015 May 12. PMID: 25825265; PMCID: PMC4507164.
In vitro protocol:
1. Lee SU, Ahn KS, Sung MH, Park JW, Ryu HW, Lee HJ, Hong ST, Oh SR. Indacaterol inhibits tumor cell invasiveness and MMP-9 expression by suppressing IKK/NF-κB activation. Mol Cells. 2014 Aug;37(8):585-91. doi: 10.14348/molcells.2014.0076. Epub 2014 Aug 18. PMID: 25134539; PMCID: PMC4145369. 2. Scola AM, Loxham M, Charlton SJ, Peachell PT. The long-acting beta-adrenoceptor agonist, indacaterol, inhibits IgE-dependent responses of human lung mast cells. Br J Pharmacol. 2009 Sep;158(1):267-76. doi: 10.1111/j.1476-5381.2009.00178.x. Epub 2009 Apr 9. PMID: 19371332; PMCID: PMC2795262.
In vivo protocol:
1. Rinaldi B, Donniacuo M, Sodano L, Gritti G, Martuscelli E, Orlandi A, Rafaniello C, Rossi F, Calzetta L, Capuano A, Matera MG. Effects of chronic treatment with the new ultra-long-acting β2 -adrenoceptor agonist indacaterol alone or in combination with the β1 -adrenoceptor blocker metoprolol on cardiac remodelling. Br J Pharmacol. 2015 Jul;172(14):3627-37. doi: 10.1111/bph.13148. Epub 2015 May 12. PMID: 25825265; PMCID: PMC4507164.