Formoterol Hemifumarate

Catalog No.S2020 Synonyms: Eformoterol, CGP 25827A, NSC 299587, YM 08316

Formoterol Hemifumarate Chemical Structure

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).

Size Price Stock Quantity  
In DMSO USD 120 In stock
USD 90 In stock
USD 370 In stock
USD 670 In stock

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Notes:

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3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

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).
Targets
β2-adrenergic receptor [1]
In vitro

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. [1] 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. [2]

In vivo Formoterol causes dose-related inhibition of histamine-induced bronchoconstriction in conscious guinea-pigs. [2] 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. [3]

Protocol

Solubility (25°C)

In vitro DMSO 80 mg/mL (198.8 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 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.

Chemical Information

Molecular Weight 402.40
Formula

C19H24N2O4.1/2C4H4O4

CAS No. 43229-80-7
Storage powder
in solvent
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

Tech Support

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Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID