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| 10mg |
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| 25mg |
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Purity: ≥98%
Formoterol (also named as Arformoterol) 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.
| Targets |
Beta-2 adrenergic receptor ( Kd = 2.9 nM )
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| ln Vitro |
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| ln Vivo |
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| 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.
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| Animal Protocol |
C57BL/6 male mice (8 wk old)
10 ng in 0.1 ml saline/20 g body weight instilled drop-wise in the external nares |
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| References | ||
| Additional Infomation |
Arformoterol Tartrate is the tartrate salt of arformoterol, the (R,R)-enantiomer of formoterol and a long-acting beta-2 adrenergic agonist with bronchodilator activity. Arformoterol selectively binds to and activates beta-2 adrenergic receptors in bronchiolar smooth muscle, thereby causing stimulation of adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased intracellular cAMP levels cause relaxation of bronchial smooth muscle and lead to an inhibition of release of inflammatory mediators from mast cells. This may eventually lead to an improvement of airway function.
See also: Arformoterol (has active moiety). |
| Molecular Formula |
C23H30N2O10
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|---|---|
| Molecular Weight |
494.5
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| Exact Mass |
494.19
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| Elemental Analysis |
C, 55.87; H, 6.12; N, 5.67; O, 32.35
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| CAS # |
200815-49-2
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| Related CAS # |
Formoterol fumarate; 43229-80-7; Arformoterol; 67346-49-0; Arformoterol maleate; 1254575-18-2
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| PubChem CID |
9827062
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| Appearance |
Solid powder
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| Boiling Point |
603.2ºC at 760mmHg
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| Vapour Pressure |
2.12E-15mmHg at 25°C
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| LogP |
1.2
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
35
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| Complexity |
521
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C[C@@H](NC[C@H](O)C1=CC(NC=O)=C(O)C=C1)CC2=CC=C(OC)C=C2.O=C(O)[C@H](O)[C@@H](O)C(O)=O
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| InChi Key |
FCSXYHUNDAXDRH-OKMNHOJOSA-N
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| InChi Code |
InChI=1S/C19H24N2O4.C4H6O6/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;5-1(3(7)8)2(6)4(9)10/h3-8,10,12-13,19-20,23-24H,9,11H2,1-2H3,(H,21,22);1-2,5-6H,(H,7,8)(H,9,10)/t13-,19+;1-,2-/m11/s
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| Chemical Name |
(2R,3R)-2,3-dihydroxybutanedioic acid;N-[2-hydroxy-5-[(1R)-1-hydroxy-2-[[(2R)-1-(4-methoxyphenyl)propan-2-yl]amino]ethyl]phenyl]formamide
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| Synonyms |
Formoterol; arformoterol; (R,R)-Formoterol; BD 40A; eformoterol; Foradil; formoterol fumarate; Trade names: Atock; Atimos/Atimos Modulite; Foradil/Foradile; Oxeze/Oxis; Perforomist
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
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| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0222 mL | 10.1112 mL | 20.2224 mL | |
| 5 mM | 0.4044 mL | 2.0222 mL | 4.0445 mL | |
| 10 mM | 0.2022 mL | 1.0111 mL | 2.0222 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00583947 | Completed | Drug: arformoterol Drug: levalbuterol |
Asthma | Sumitomo Pharma America, Inc. | January 2008 | Phase 2 |
| NCT00773786 | Completed | Drug: Arformoterol (Brovana) Drug: Placebo |
COPD | Trinity Health Of New England | October 2008 | Phase 4 |
| NCT00064415 | Completed | Drug: arformoterol Drug: Salmeterol |
Emphysema Chronic Bronchitis |
Sumitomo Pharma America, Inc. | June 2002 | Phase 3 |
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