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Submit ReviewFormoterol 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).
Formoterol hemifumarate is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 402.45 |
公式 | C19H24N2O4.½C4H4O4 |
储存 | Store at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 43229-80-7 |
PubChem ID | 9832292 |
InChI Key | OBRNDARFFFHCGE-PERKLWIXSA-N |
Smiles | [H]OC(=O)\C=C\C(=O)O[H].COC1=CC=C(C=C1)C[C@H](C)NC[C@@H](O)C1=CC(NC([H])=O)=C(O)C=C1.COC1=CC=C(C=C1)C[C@H](C)NC[C@@H](O)C1=CC(NC([H])=O)=C(O)C=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 50 |
以下数据基于产品分子量 402.45。 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.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 4.97 mL | 24.85 mL | 49.7 mL |
2.5 mM | 0.99 mL | 4.97 mL | 9.94 mL |
5 mM | 0.5 mL | 2.48 mL | 4.97 mL |
25 mM | 0.1 mL | 0.5 mL | 0.99 mL |
参考文献是支持产品生物活性的出版物。
Anderson (1993) Formoterol: pharmacology, molecular basis of agonism, and mechanism of long duration of a highly potent and selective β2-adrenoceptor agonist bronchodilator. Life Sci. 52 2145 PMID: 8099696
Decker et al (1982) Effects of N-aralkyl substitution of β-agonists on α- and β-adrenoceptor subtypes: pharmacological studies and binding assays. J.Pharm.Pharmacol. 34 107 PMID: 6121868
Naline et al (1994) Relaxant effects and durations of action of formo. and salme. on the isolated human bronchus. Eur.Respir.J. 7 914 PMID: 7914176
If you know of a relevant reference for Formoterol hemifumarate, please let us know.
关键词: Formoterol hemifumarate, Formoterol hemifumarate supplier, Potent, selective, β2-adrenoceptor, α2-adrenoceptor, beta2-adrenoceptor, b2-adrenoceptor, β2-adrenergic, α2-adrenergic, beta2-adrenergic, b2-adrenergic, agonists, Receptors, BD40A, BD, 40A, Adrenergic, Beta-2, 1448, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Formoterol hemifumarate 的部分引用包括:
McKeithan et al (2017) An Automated Platform for Assessment of Congenital and Drug-Induced Arrhythmia with hiPSC-Derived Cardiomyocytes. Front Physiol 8 766 PMID: 29075196
Lavine et al (2013) Attenuation of choroidal neovascularization by β(2)-adrenoreceptor antagonism. JAMA Ophthalmol 131 376 PMID: 23303344
Bacou (2017) β2-adrenoreceptor stimulation dampens the LPS-induced M1 polarization in pig macrophages. Dev Comp Immunol 76 169 PMID: 28633932
Luo (2017) β2-adrenoreceptor Inverse Agonist Down-regulates Muscarine Cholinergic Subtype-3 Receptor and Its Downstream Signal Pathways in Airway Smooth Muscle Cells in vitro. Scientific Reports 7 39905 PMID: 28051147
Lavine (2017) β2-Adrenergic Receptor Antagonism Attenuates CNV Through Inhibition of VEGF and IL-6 Expression. Invest Ophthalmol Vis Sci 58 299 PMID: 28114591
Koziczak-Holbro et al (2019) 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. J Pharmacol Exp Ther 369 188 PMID: 30819762
Pon et al (2016) The β2-adrenoceptor activates a positive cAMP-calcium feedforward loop to drive breast cancer cell invasion. FASEB J 30 1144 PMID: 26578688
Liu et al (2015) 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. Mol Cell Neurosci 11 4121 PMID: 25672589
Maupoil et al (2007) Ectopic activity in the rat pulmonary vein can arise from simultaneous activation of alpha1- and beta1-adrenoceptors. Br J Pharmacol 150 899 PMID: 17325650
Plummer et al (2004) Expression of inwardly rectifying potassium channels (GIRKs) and beta-adrenergic regulation of breast cancer cell lines. BMC Cancer 4 93 PMID: 15603589
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.