Formoterol maleate is a long-acting β2 agonist (LABA) used in the treatment of asthma and COPD (chronic obstructive pulmonary disease). It is sold under several trade names, such as Atock, Atimos/Atimos Modulite, Foradil/Foradile, Oxeze/Oxis, and Perforomist, in three different forms: a dry powder inhaler, a metered-dose inhaler, and an inhalation solution. The combination formulations of mometasone/formoterol and budesonide/formoterol are also available for purchase. Compared to short-acting β2 agonists like salbutamol (albuterol), which have an efficacious duration of 4–6 hours, formoterol exhibits an extended duration of action (up to 12 hours). LABAs, like formoterol, are used in addition to prophylactic corticosteroid therapy as "symptom controllers." Since LABAs are not advised for the treatment of acute asthma, a "reliever" short-acting β2 agonist (such as salbutamol) is still needed.

Physicochemical Properties

Molecular Formula	C23H28N2O8
Molecular Weight	460.477026939392
Exact Mass	460.18
Elemental Analysis	C, 59.99; H, 6.13; N, 6.08; O, 27.80
CAS #	1254575-18-2
Related CAS #	Arformoterol; 67346-49-0; Formoterol-1; 73573-87-2; (S,S)-Formoterol; 67346-48-9; Arformoterol tartrate; 200815-49-2
PubChem CID	49821151
Appearance	Solid powder
Hydrogen Bond Donor Count	6
Hydrogen Bond Acceptor Count	9
Rotatable Bond Count	10
Heavy Atom Count	33
Complexity	507
Defined Atom Stereocenter Count	2
SMILES	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
InChi Key	ZDUPYZMAPCZGJO-QVVSPZKGSA-N
InChi Code	InChI=1S/C19H24N2O4.C4H4O4/c1-13(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/h3-8,10,12-13,19-20,23-24H,9,11H2,1-2H3,(H,21,22);1-2H,(H,5,6)(H,7,8)/b;2-1-/t13-,19+;/m1./s1
Chemical Name	(Z)-but-2-enedioic acid;N-[2-hydroxy-5-[(1R)-1-hydroxy-2-[[(2R)-1-(4-methoxyphenyl)propan-2-yl]amino]ethyl]phenyl]formamide
Synonyms	Arformoterol Maleate; (-)-Formoterol; Arformoterol; (R,R)-Formoterol Maleate; Formoterol; arformoterol; (R,R)-Formoterol; BD 40A; eformoterol; Foradil; Trade names: Atock, Atimos/Atimos Modulite, Foradil/Foradile; Oxeze/Oxis; Perforomist
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	Beta-2 adrenergic receptor ( Kd = 2.9 nM )
ln Vitro	In vitro activity: Arformoterol causes the accumulation of cAMP in human bronchial epithelial cells in culture[1].
ln Vivo	Arformoterol (10 ng in 0.1 ml saline/20 g body weight; intranasal instillation) reduces the respiratory system elastance and resistance that Cl2-induced increases in mice exhibit[3]. Arformoterol reverses the bronchoconstriction caused by ovalbumin and histamine in guinea pigs (ED50s=1 and 40 nmol/kg, respectively)[1].
Enzyme Assay	Formoterol(Arformoterol) is a brand-new, highly selective β2-adrenergic agonist that shows potential as a β2-agonist with selectively advantageous metabolic effects.
Animal Protocol	Wild-type and iNOS−/− mice were exposed to Cl2 gas 10 ng in 0.1 ml saline/20 g body weight Intranasal instillation in the external nares at 10 minutes and every 24 hours after exposure
References	[1]. Biological actions of formoterol isomers. Pulm Pharmacol Ther. 2002;15(2):135-45. [2]. Arformoterol tartrate in the treatment of COPD. Expert Rev Respir Med. 2010 Apr;4(2):155-62. [3]. Postexposure administration of a {beta}2-agonist decreases chlorine-induced airway hyperreactivity in mice. Am J Respir Cell Mol Biol. 2011 Jul;45(1):88-94.

Solubility Data

Solubility (In Vitro)

DMSO: ≥ 50 mg/mL Water: < 1 mg/mL Ethanol: N/A

Solubility (In Vivo)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.1716 mL	10.8582 mL	21.7165 mL
	5 mM	0.4343 mL	2.1716 mL	4.3433 mL
	10 mM	0.2172 mL	1.0858 mL	2.1716 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.