Formoterol Hemifumarate

Synonyms: Eformoterol, CGP 25827A, NSC 299587, YM 08316,Formoterol fumarate

Formoterol Hemifumarate (Eformoterol, CGP 25827A, NSC 299587, YM 08316,Formoterol fumarate) is a potent, selective and long-acting β2-adrenoceptor agonist used in the management of asthma and chronic obstructive pulmonary disease(COPD).

Formoterol Hemifumarate Chemical Structure

Formoterol Hemifumarate Chemical Structure

CAS No. 43229-80-7

Purity & Quality Control

Formoterol Hemifumarate Related Products

Biological Activity

Description Formoterol Hemifumarate (Eformoterol, CGP 25827A, NSC 299587, YM 08316,Formoterol fumarate) 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
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
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]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06102005 Recruiting
Asthma
Sanofi
October 16 2023 Phase 2
NCT05421598 Active not recruiting
Asthma
Sanofi
June 30 2022 Phase 2
NCT04663386 Terminated
Asthma|COPD
Orion Corporation Orion Pharma
December 10 2020 --

Chemical Information & Solubility

Molecular Weight 402.40 Formula

C19H24N2O4.1/2C4H4O4

CAS No. 43229-80-7 SDF Download Formoterol Hemifumarate SDF
Smiles CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O.CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 80 mg/mL ( (198.8 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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