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| 25mg |
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Formoterol fumarate dihydrate (also known as Foradil) is a long-acting β2 agonist (LABA) used in the treatment of asthma and COPD (chronic obstructive pulmonary disease). It is marketed in three forms: a dry-powder inhaler, a metered-dose inhaler and an inhalation solution, under various trade names including Atock, Atimos/Atimos Modulite, Foradil/Foradile, Oxeze/Oxis, and Perforomist. Mometasone/formoterol and Budesonide/formoterol combination formulations are also available for purchase. Unlike salbutamol (albuterol), which acts for 4 to 6 hours, formoterol acts for up to 12 hours. This is a longer duration of action than other short-acting β2 agonists. In addition to prophylactic corticosteroid therapy, LABAs like formoterol are used as "symptom controllers." When treating acute asthma, LABAs are not advised; instead, a "reliever" short-acting β2 agonist (such as salbutamol) is still needed.
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Formoterol((also known as arformoterol) exhibits great potential as a β2-agonist that may provide desired metabolic effects with its unique and highly β2-selective adrenergic agonist properties.
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| References |
| Molecular Formula |
2(C19H24N2O4).C4H4O4.2(H2O)
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| Molecular Weight |
496.51
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| CAS # |
183814-30-4
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| Related CAS # |
Formoterol fumarate; 43229-80-7
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| SMILES |
CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O.CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O.C(=C/C(=O)O)\C(=O)O.O.O
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| InChi Key |
RATSWNOMCHFQGJ-XODSYJLDSA-N
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| InChi Code |
InChI=1S/2C19H24N2O4.C4H4O4.2H2O/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);2*1H2/b;;2-1+;;
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| Chemical Name |
(E)-but-2-enedioic acid;N-[2-hydroxy-5-[1-hydroxy-2-[1-(4-methoxyphenyl)propan-2-ylamino]ethyl]phenyl]formamide;dihydrate
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| Synonyms |
(-)-Formoterol; Arformoterol; (R,R)-Formoterol; 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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| 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 | 2.0141 mL | 10.0703 mL | 20.1406 mL | |
| 5 mM | 0.4028 mL | 2.0141 mL | 4.0281 mL | |
| 10 mM | 0.2014 mL | 1.0070 mL | 2.0141 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 |
| NCT05831566 | Recruiting | Drug: Budesonide/Formoterol fumarate dihydrate |
Asthma | Franciscus Gasthuis | January 31, 2023 | Phase 3 |
| NCT02495168 | Completed | Drug: Generic Budesonide/ Formoterol Fumarate Dihydrate |
Asthma | Actavis Inc. | January 13, 2017 | Phase 3 |
| NCT05322707 | Completed | Drug: Placebo Drug: Symbicort, 80 Mcg- 4.5 Mcg/Inh Inhalation Aerosol |
Asthma | Cipla Ltd. | April 15, 2022 | Phase 3 |
| NCT03015259 | Completed | Drug: Symbicort Drug: Placebo |
Asthma | Kindeva Drug Delivery | December 29, 2016 | Phase 3 |
| NCT02384577 | Completed | Drug: Budesonide, Formoterol Fumarate Dihydrate |
Patient Satisfaction | Teva Pharma GmbH/td> | July 2014 | N/A |
% predicted FEV1at different time points in the 2 groups.BMC Pediatr.2012 Mar 7;12:21. |
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Chlorine (Cl2) exposure increases respiratory resistance and elastance, which are mitigated by arformoterol (Arfor).Am J Respir Cell Mol Biol. 2011 Jul; 45(1): 88–94. |
Lung histology after Cl2exposure and treatment of Arfor: Airway cross-sections of mice breathing air (A), or exposed to Cl2treated with saline (B) or Arfor (C),Am J Respir Cell Mol Biol. 2011 Jul; 45(1): 88–94. |
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