Formoterol (Fumarate)

Cas No.:	43229-80-7
Chemical Name:	(E)-but-2-enedioic acid;N-[2-hydroxy-5-[(1R)-1-hydroxy-2-[[(2R)-1-(4-methoxyphenyl)propan-2-yl]amino]ethyl]phenyl]formamide
Synonyms:	Formoterol Fumarate; Aformoterol; CHEBI:63108; Atock; Foradil Aerolizer; Foradil formoterol, ((R*,R*)-(±))-isomer; Oxis; formoterol fumarate, ((R*,R*)-(±))-isomer;
SMILES:	C[C@@H](CC1=CC=C(C=C1)OC)NC[C@H](C2=CC(=C(C=C2)O)NC=O)O.C[C@@H](CC1=CC=C(C=C1)OC)NC[C@H](C2=CC(=C(C=C2)O)NC=O)O.C(=C/C(=O)O)\C(=O)O
Formula:	C23H28N2O8
M.Wt:	460.48
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Formoterol fumarate(Foradil) is a potent, selective and long-acting β2-adrenoceptor agonist.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].
Target:	.IC50 Value: 2.1 nM in pregnant C3H/HeN strain mice[5] Target: β2 receptor
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
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].
References:	[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.