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Formoterol (fumarate)

Formoterol fumarate (Formoterol) is a potent, selective and long-acting β2-adrenoceptor agonist. IC50 Value: 2.1 nM in pregnant C3H/HeN strain mice[5] Target: β2 receptor Budesonide/formoterol in a single inhaler for both maintenance and reliever therapy is now an established therapeutic option for management of inadequately controlled asthma[4]. in vitro:. The long-acting β (2) -agonist formoterol and the glucocorticoid dexamethasone significantly reduced HRV-induced ERK phosphorylation, Fra-1, and MMP-9 expression in BEAS-2B cells[3]. in vivo: compared the bronchodilatory effects of inhaled budesonide/formoterol (dose: 200 μg and 12 μg respectively) combination with budesonide (200 μg) /salbutamol (200 μg) administered by metered dose inhaler and spacer in children of 5-15 years with mild acute exacerbation of asthma [Modified Pulmonary Index Score (MPIS) between 6-8] in this double-blind, randomized controlled trial. The primary outcome was FEV1 (% predicted) in the two groups at 1, 5, 15, 30, 60 min after administration of the study drug[1]. Fifteen randomized, placebo-controlled clinical trials including COPD patients were evaluated: indacaterol 75 μg once daily (n = 2 studies), indacaterol 150 μg once daily (n = 5), indacaterol 300 μg once daily (n = 4), FOR/BUD 9/160 μg twice daily (n = 2), FOR/BUD 9/320 μg twice daily (n = 2), SAL/FP 50/500 μg twice daily (n = 4), and SAL/FP 50/250 μg twice daily (n = 1) [2]. Clinical trial: Effects of Mometasone Furoate/Formoterol Combination Versus Mometasone Furoate Alone in Persistent Asthmatics (Study P04073) . Phage3

Product Specifications

CAS Number

[43229-80-7]

Product Name Alternative

(±) Formoterol (fumarate)

UNSPSC

12352211

Hazard Statement

H332, H351, H361, H370, H372

Target

Adrenergic Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Endocrinology

Concentration

10mM

Purity

99.95

Solubility

DMSO : ≥ 50 mg/mL|H2O : < 0.1 mg/mL

Smiles

O=CNC1=CC([C@@H](O)CN[C@H](C)CC2=CC=C(OC)C=C2)=CC=C1O.O=C(O)/C=C/C(O)=O.[1/2]

Molecular Formula

C19H24N2O4.1/2C4H4O4

Molecular Weight

402.44

Precautions

H332, H351, H361, H370, H372

References & Citations

[1]Arun JJ, Lodha R, Kabra SK. Bronchodilatory effect of inhaled budesonide/formoterol and budesonide/salbutamol in acute asthma: a double-blind, randomized controlled trial.BMC Pediatr. 2012 Mar 7;12:21.|[2]Cope S, Kraemer M, Zhang J, Efficacy of indacaterol 75 μg versus fixed-dose combinations of formoterol-budesonide or salmeterol-fluticasone for COPD: a network meta-analysis. Int J Chron Obstruct Pulmon Dis. 2012;7:415-20.|[3]Tacon CE, Newton R, Proud D, Rhinovirus-induced MMP-9 expression is dependent on Fra-1, which is modulated by formoterol and dexamethasone. J Immunol. 2012 May 1;188 (9) :4621-30.|[4]Zhong N, Lin J, Mehta P, Real-life effectiveness of budesonide/formoterol maintenance and reliever therapy in asthma patients across Asia: SMARTASIA study. BMC Pulm Med. 2013 Apr 4;13 (1) :22.|[5]Shinkai N, Takasuna K, Takayama S. Tocolytic activity of formoterol against premature delivery in mice. J Pharm Pharmacol. 2002 Dec;54 (12) :1637-43.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Launched

Available Sizes

Curated Selection

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