Name: Indacaterol Maleate
Brand: Selleck Chemicals
SKU: S3083
Availability: InStock
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Quality Control

Batch: S308301 DMSO]102 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.88%

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COA
NMR
SDS
Datasheet

99.88

Related Targets	AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Adrenergic Receptor Products	Zenidolol (ICI-118551) Hydrochloride Yohimbine HCl L755507 Atipamezole Higenamine hydrochloride Fenoterol hydrobromide Medetomidine HCl Rauwolscine hydrochloride Deoxycorticosterone acetate Detomidine HCl

Solubility

In vitro
Batch:

DMSO : 102 mg/mL (200.56 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight	508.56	Formula	C₂₄H₂₈N₂O₃.C₄H₄O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	753498-25-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	QAB149			Smiles	CCC1=C(C=C2CC(CC2=C1)NCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)CC.C(=CC(=O)O)C(=O)O

Mechanism of Action

Targets/IC₅₀/Ki	β1-adrenoceptor 7.36(pKi) β2-adrenoceptor 5.48(pKi)
In vitro	Indacaterol induces cAMP production in Chinese hamster ovary cells stably transfected with human β2 adrenoceptors. It inhibits electrically induced contraction on the electrically stimulated guinea pig trachea in a concentration-dependent manner with pEC50 of 8.23. Indacaterol induces a concentration-dependent inotropic effect with maximal efficacy of 75% in the isolated guinea pig left atrium. Indacaterol reverses the carbachol-induced contraction in a concentration-dependent manner with IC50 of 37 nM in human small airways. Indacaterol concentration dependently reverses the serotonin-induced contraction with IC50 of 10.5 nM in rat small airways. Indacaterol has the highest intrinsic efficacy of 53% in rat small airways and 73% in human small airways. Indacaterol (10 μM) induces close to full inhibition of the EFS-induced contraction of isolated human bronchi and the effect lasts 12 hours. Indacaterol inhibits the IgE-dependent release of histamine from mast cells with the intrinsic activity (Emax of a long-acting Indacaterol/Emax of Isoprenaline) of 1.03. Indacaterol induces cAMP production from human airway smooth muscle with pEC50 of 8.53 and Emax of 48%. Indacaterol appears to have a reduced efficacy compared with the CHO-K1 data in the primary ASM cells.
In vivo	Indacaterol (6.7 μg/kg) inhibits 5-HT-induced bronchoconstriction with a maximal effect of 85% in the conscious guinea pig. Indacaterol (12.5 μg/kg) dose-dependently inhibits methacholine-induced bronchoconstriction with a maximal effect of 85% in the anesthetized rhesus monkey.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16434564/ [2] https://pubmed.ncbi.nlm.nih.gov/17916760/ [3] https://pubmed.ncbi.nlm.nih.gov/17135231/ [4] https://pubmed.ncbi.nlm.nih.gov/19371332/ [5] https://pubmed.ncbi.nlm.nih.gov/19422388/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05288075	Completed	Healthy Volunteers	Orion Corporation Orion Pharma	February 28 2022	Phase 1
NCT03030638	Completed	Pulmonary Disease Chronic Obstructive	Boehringer Ingelheim\|RTI health solutions US	February 8 2017	--

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Indacaterol Maleate Adrenergic Receptor agonist

Chemical Structure

Molecular Weight: 508.56