Formoterol fumarate

Formoterol Fumarate is a potent β-AR adrenoceptor agonist with a prolonged duration of action. This compound demonstrates a 330-fold selectivity for β2 over β1 receptors. Formoterol Fumarate has been reported to be 150-200 times more potent than isoprenaline. This agent has also been noted to reduce the loss of muscle mass in murine models. And, it is used to manage asthma and in the treatment of chronic obstructive pulmonary disease.

Product information

CAS Number: 43229-80-7

Molecular Weight: 402.44

Formula: C42H52N4O12

Synonym:

Foradil

Chemical Name: (2E)-but-2-enedioic acid; bis(N-{2-hydroxy-5-[(1S)-1-hydroxy-2-{[(2S)-1-(4-methoxyphenyl)propan-2-yl]amino}ethyl]phenyl}formamide)

Smiles: C[C@@H](CC1C=CC(=CC=1)OC)NC[C@@H](O)C1=CC(NC=O)=C(O)C=C1.C[C@@H](CC1C=CC(=CC=1)OC)NC[C@@H](O)C1=CC(NC=O)=C(O)C=C1.OC(=O)/C=C/C(O)=O

InChiKey: OBRNDARFFFHCGE-PERKLWIXSA-N

InChi: InChI=1S/2C19H24N2O4.C4H4O4/c2*1-13(9-14-3-6-16(25-2)7-4-14)20-11-19(24)15-5-8-18(23)17(10-15)21-12-22;5-3(6)1-2-4(7)8/h2*3-8,10,12-13,19-20,23-24H,9,11H2,1-2H3,(H,21,22);1-2H,(H,5,6)(H,7,8)/b;;2-1+/t2*13-,19+;/m00./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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.

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.
3. Whelan CJ, et al. Br J Pharmacol, 1993, 110(2), 613-618.

Products are for research use only. Not for human use.