Formoterol Hemifumarate

Catalog No.S2020

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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Formoterol Hemifumarate Chemical Structure

Formoterol Hemifumarate Chemical Structure
Molecular Weight: 402.40

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Formoterol Hemifumarate is available in the following compound libraries:

Product Information

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Product Description

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]
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Anderson GP, et al. Life Sci, 1993, 52(26), 2145-2160.

[2] Nials AT, et al. Eur J Pharmacol, 1994, 251(2-3), 127-135.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-04-18)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02415179 Not yet recruiting Asthma Mahidol University May 2015 --
NCT02291016 Recruiting COPD Exacerbation University of Tennessee Graduate School of Medicine|Myla  ...more University of Tennessee Graduate School of Medicine|Mylan Specialty L.P. February 2015 --
NCT02345161 Recruiting Pulmonary Disease, Chronic Obstructive GlaxoSmithKline January 2015 Phase 3
NCT02345993 Active, not recruiting Asthma|Asthmatic Crisis National Institute of Respiratory Diseases, Mexico January 2015 Phase 4
NCT02308098 Recruiting Asthma Orion Corporation, Orion Pharma December 2014 Phase 3

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Chemical Information

Download Formoterol Hemifumarate SDF
Molecular Weight (MW) 402.40
Formula

C19H24N2O4.1/2C4H4O4

CAS No. 43229-80-7
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms Eformoterol, CGP 25827A, NSC 299587, YM 08316
Solubility (25°C) * In vitro DMSO 80 mg/mL (198.8 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
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 Name N-(2-hydroxy-5-((S)-1-hydroxy-2-((S)-1-(4-methoxyphenyl)propan-2-ylamino)ethyl)phenyl)formamide hemifumaric acid

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