Catalog No.S2020 Synonyms: Eformoterol, CGP 25827A, NSC 299587, YM 08316
Molecular Weight(MW): 402.40
Formoterol Hemifumarate is a potent, selective and long-acting β2-adrenoceptor agonist used in the management of asthma and chronic obstructive pulmonary disease(COPD).
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|Description||Formoterol Hemifumarate is a potent, selective and long-acting β2-adrenoceptor agonist used in the management of asthma and chronic obstructive pulmonary disease(COPD).|
Formoterol is a potent airway smooth muscle relaxant with high efficacy, and very high affinity and selectivity for the beta 2-adrenoceptor. Formoterol appears to be retained in airway smooth muscle for extended periods since its relaxant effect on human airway smooth muscle is resistant to repeated washing and formoterol displays 'reassertion' of relaxation after washout of a beta-adrenoceptor antagonist. Formoterol has been demonstrated to potently inhibit these cells and processes in experimental test systems.  Formoterol, like salbutamol and salmeterol, relaxes isolated preparations of guinea-pig trachea and human bronchus, and inhibits antigen-induced mediator release from human lung fragments in a concentration-related fashion. 
|In vivo||Formoterol causes dose-related inhibition of histamine-induced bronchoconstriction in conscious guinea-pigs.  Formoterol inhibits histamine-induced plasma protein extravasation (PPE) in guinea-pig lung, with significant inhibition being observed at 10 mg /mL and 100 mg /mL. Formoterol (100 mg /mL) inhibits PPE in guinea-pig lung for 2-4 hours, a duration of action intermediate between that previously obtained for salbutamol (1 hour) and salmeterol (> 6 hours). Formoterol inhibits neutrophil accumulation (lipopolysaccharide-induced) in guinea-pig lung but at doses greater than those required to inhibit granulocyte-independent PPE (histamine-induced). Formoterol (100 mg /mL) inhibits PAF-induced eosinophil accumulation in guinea-pig lung. |
|In vitro||DMSO||80 mg/mL (198.8 mM)|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||Eformoterol, CGP 25827A, NSC 299587, YM 08316|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02796677||Recruiting||Chronic Obstructive Pulmonary Disease||AstraZeneca||July 2016||Phase 3|
|NCT02787967||Not yet recruiting||Asthma||Chiesi Farmaceutici S.p.A.||June 2016||Phase 2|
|NCT02796651||Recruiting||Chronic Obstructive Pulmonary Disease (COPD)||AstraZeneca|Parexel||June 2016||Phase 2|
|NCT02757209||Recruiting||Asthma|COPD||Consorzio Futuro in Ricerca||April 2016||Phase 4|
|NCT02753712||Not yet recruiting||Asthma||Mundipharma Research Limited||April 2016||Phase 3|
|NCT02693769||Not yet recruiting||ACOS (Fixed Airflow Obstruction and Elevated Eosinophils)||Mundipharma Research Limited||March 2016||Phase 2|Phase 3|
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