Formoterol hemifumarate
Chemical Name: (±)-(R,R)-N-[2-Hydroxy-5-[1-hydroxy-2-[[2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]phenyl] formamide hemifumarate
Purity: ≥99%
Biological Activity
Formoterol hemifumarate is a potent, selective and long-acting β2-adrenoceptor agonist. Displays 330-fold selectivity for β2 over β1 receptors (pKd values are 8.12 and 5.58 respectively). Potently relaxes guinea pig trachea (pD2 = 9.29), and is longer-acting and 100-fold more potent than Salbutamol (Cat. No. 0634).Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Effects of N-aralkyl substitution of β-agonists on α- and β-adrenoceptor subtypes: pharmacological studies and binding assays.
Decker et al.
J.Pharm.Pharmacol., 1982;34:107 -
Formoterol: pharmacology, molecular basis of agonism, and mechanism of long duration of a highly potent and selective β2-adrenoceptor agonist bronchodilator.
Anderson
Life Sci., 1993;52:2145 -
Relaxant effects and durations of action of formo. and salme. on the isolated human bronchus.
Naline et al.
Eur.Respir.J., 1994;7:914
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Citations for Formoterol hemifumarate
The citations listed below are publications that use Tocris products. Selected citations for Formoterol hemifumarate include:
10 Citations: Showing 1 - 10
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Pharmacological Characterization of a Novel 5-Hydroxybenzothiazolone-Derived β2-Adrenoceptor Agonist with Functional Selectivity for Anabolic Effects on Skeletal Muscle Resulting in a Wider Cardiovascular Safety Window in Preclinical Studies.
Authors: Koziczak-Holbro Et al.
J Pharmacol Exp Ther 2019;369:188
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An Automated Platform for Assessment of Congenital and Drug-Induced Arrhythmia with hiPSC-Derived Cardiomyocytes.
Authors: McKeithan Et al.
Front Physiol 2017;8:766
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β2-adrenoreceptor Inverse Agonist Down-regulates Muscarine Cholinergic Subtype-3 Receptor and Its Downstream Signal Pathways in Airway Smooth Muscle Cells in vitro.
Authors: Luo
Scientific Reports 2017;7:39905
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β2-adrenoreceptor stimulation dampens the LPS-induced M1 polarization in pig macrophages.
Authors: Bacou
Dev Comp Immunol 2017;76:169
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β2-Adrenergic Receptor Antagonism Attenuates CNV Through Inhibition of VEGF and IL-6 Expression.
Authors: Lavine
Invest Ophthalmol Vis Sci 2017;58(1):299
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The β2-adrenoceptor activates a positive cAMP-calcium feedforward loop to drive breast cancer cell invasion.
Authors: Pon Et al.
FASEB J 2016;30:1144
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A long-acting β2-adrenergic agonist increases the expression of muscarine cholinergic subtype-3 receptors by activating the β2-adrenoceptor cyclic adenosine monophosphate signaling pathway in airway smooth muscle cells.
Authors: Liu Et al.
Mol Cell Neurosci 2015;11:4121
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Attenuation of choroidal neovascularization by β(2)-adrenoreceptor antagonism.
Authors: Lavine Et al.
JAMA Ophthalmol 2013;131:376
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Ectopic activity in the rat pulmonary vein can arise from simultaneous activation of alpha1- and beta1-adrenoceptors.
Authors: Maupoil Et al.
Br J Pharmacol 2007;150:899
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Expression of inwardly rectifying potassium channels (GIRKs) and beta-adrenergic regulation of breast cancer cell lines.
Authors: Plummer Et al.
BMC Cancer 2004;4:93
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