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product name Formoterol Hemifumarate


Description: Formoterol Hemifumarate (Eformoterol, CGP 25827A, NSC 299587, YM 08316) 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. 

References: Life Sci. 1993;52(26):2145-60; Eur J Pharmacol. 1994 Jan 14;251(2-3):127-35.



Molecular Weight (MW)

402.40 
Formula

C19H24N2O4.1/2C4H4O4 
CAS No.

43229-80-7 
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

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

 
Synonyms

Eformoterol, CGP 25827A, NSC 299587, YM 08316 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19398555

In Vitro

In vitro activity: 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.


Kinase Assay:


Cell Assay

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. 
Animal model  
Formulation & Dosage  
References Life Sci. 1993;52(26):2145-60; Eur J Pharmacol. 1994 Jan 14;251(2-3):127-35. 

BAY 41-2272

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Author: Sodium channel

Share this post on:

product name Formoterol Hemifumarate


Description: Formoterol Hemifumarate (Eformoterol, CGP 25827A, NSC 299587, YM 08316) 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. 

References: Life Sci. 1993;52(26):2145-60; Eur J Pharmacol. 1994 Jan 14;251(2-3):127-35.



Molecular Weight (MW)

402.40 
Formula

C19H24N2O4.1/2C4H4O4 
CAS No.

43229-80-7 
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

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

 
Synonyms

Eformoterol, CGP 25827A, NSC 299587, YM 08316 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19398555

In Vitro

In vitro activity: 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.


Kinase Assay:


Cell Assay

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. 
Animal model  
Formulation & Dosage  
References Life Sci. 1993;52(26):2145-60; Eur J Pharmacol. 1994 Jan 14;251(2-3):127-35. 

BAY 41-2272

Share this post on:

Author: Sodium channel