| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
β₂-Adrenergic Receptor (β₂-AR) (EC₅₀=0.25 nM for cAMP accumulation in human β₂-AR-expressing cells) [1]
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| ln Vitro |
In vitro activity: Formoterol inhibited the phosphorylation of JNK1 and GR-Ser226, which restored Dex sensitivity. Partially inhibiting H(2) O(2)-induced PI3Kδ-dependent (PKB) phosphorylation was formoterol (FM), but not SM. H(2) O(2) lowered the amount of cAMP produced in U937 cells by SM, but had no discernible impact on the cells' reaction to FM.
Formoterol fumarate dihydrate is a long-acting, selective β₂-adrenergic receptor agonist with potent bronchodilatory and anti-inflammatory activities [1] - Relaxes isolated human tracheal smooth muscle: Concentration-dependently inhibits acetylcholine (ACh)-induced contraction with EC₅₀=0.8 nM; 10 nM achieves 92% relaxation, and the effect persists for 8–10 hours [1] - Inhibits airway smooth muscle cell (ASMC) proliferation: 0.1–10 nM Formoterol fumarate dihydrate reduces platelet-derived growth factor (PDGF)-BB-induced ASMC proliferation by 30–68% (BrdU incorporation assay), mediated by the cAMP/PKA signaling pathway [1] - Exhibits anti-inflammatory activity in human bronchial epithelial cells (HBECs): 0.01–1 nM Formoterol fumarate dihydrate dose-dependently decreases TNF-α-induced production of pro-inflammatory chemokines CXCL8 (IL-8) and CCL11 (eotaxin) by 38–62% and 32–55%, respectively [1] - No significant cytotoxicity: HBECs and ASMCs incubated with Formoterol fumarate dihydrate up to 100 nM for 72 hours show >90% cell viability (MTT assay) [1] |
| ln Vivo |
Formoterol exposure for 24 or 72 hours increased the number of copies of mtDNA in the kidney and heart, increased the number of copies of peroxisome proliferator-activated receptor γ coactivator 1α, and increased the number of genes involved in the mitochondrial electron transport chain (F0 subunit 6 of transmembrane F-type ATP synthase, NADH dehydrogenase subunit 1, NADH dehydrogenase subunit 6, and NADH dehydrogenase [ubiquinone] 1β subcomplex subunit 8). Rat uterine contraction amplitude and frequency were inhibited by formoterol and ritodrine, with IC50 values of 3.8 x 10(-10) and 4.7 x 10(-7) M, respectively.
Reduces chlorine-induced airway hyperreactivity (AHR) in mice: C57BL/6 mice exposed to chlorine gas (400 ppm for 5 minutes) were treated with Formoterol fumarate dihydrate (0.3 μg/kg, 1 μg/kg) via intraperitoneal injection 1 hour post-exposure. The 1 μg/kg dose decreases AHR to methacholine (PC₂₀=10.6 mg/mL vs 4.3 mg/mL in vehicle control, p<0.001) and reduces lung eosinophil infiltration by 58% [1] - Attenuates airway inflammation in ovalbumin (OVA)-sensitized mice: Inhaled Formoterol fumarate dihydrate (0.5 μg/kg) once daily for 7 days decreases OVA-induced peribronchial inflammation (lymphocyte/macrophage infiltration reduced by 50%) and mucus hypersecretion (MUC5AC mRNA expression reduced by 52%) [1] - Improves lung function in pediatric asthma patients: A randomized controlled trial in 42 children (6–12 years old) with mild-to-moderate asthma showed that inhaled Formoterol fumarate dihydrate (9 μg twice daily) for 12 weeks significantly improved forced expiratory volume in 1 second (FEV₁) by 14% (from 78% predicted to 92% predicted, p<0.01) and reduced asthma symptom scores (from 4.2 ± 1.1 to 1.8 ± 0.7, p<0.001) compared to placebo [2] - Reduces asthma exacerbation rate in children: The 12-week trial showed that the exacerbation rate in the Formoterol fumarate dihydrate group was 0.2 episodes per patient-year, significantly lower than the placebo group (1.1 episodes per patient-year, p<0.05) [2] |
| Enzyme Assay |
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.
β₂-AR functional assay (cAMP accumulation): Human β₂-AR-expressing CHO cells are seeded in 96-well plates and pre-incubated with serial 3-fold dilutions of Formoterol fumarate dihydrate (0.001–100 nM) for 30 minutes. IBMX (100 μM) is added to inhibit cAMP phosphodiesterase, and cells are incubated at 37°C for an additional 30 minutes. cAMP is extracted with ethanol, and concentrations are measured by ELISA. EC₅₀ values are calculated via nonlinear regression of concentration-response curves [1] |
| Cell Assay |
Tracheal smooth muscle relaxation assay: Isolated human tracheal rings are mounted in organ baths containing Krebs-Henseleit solution (37°C, bubbled with 95% O₂/5% CO₂) under a resting tension of 1 g. After 60 minutes of equilibration, rings are pre-contracted with ACh (1 μM). Cumulative concentrations of Formoterol fumarate dihydrate (0.01–100 nM) are added, and relaxation percentage is calculated relative to ACh-induced maximal contraction [1]
- ASMC proliferation assay: Human ASMCs are seeded in 96-well plates (4×10³ cells/well) and synchronized in serum-free medium for 24 hours. Cells are treated with Formoterol fumarate dihydrate (0.1–10 nM) plus PDGF-BB (10 ng/mL) and cultured for 48 hours. BrdU is added for the final 12 hours, and incorporated BrdU is detected by ELISA to quantify proliferation [1] - Chemokine expression assay: HBECs are seeded in 6-well plates (2×10⁵ cells/well) and treated with Formoterol fumarate dihydrate (0.01–1 nM) for 1 hour, then stimulated with TNF-α (10 ng/mL) for 24 hours. Culture supernatants are collected, and CXCL8/CCL11 levels are measured by ELISA [1] |
| Animal Protocol |
Chlorine-induced AHR mouse model: Female C57BL/6 mice (6–8 weeks old) are exposed to 400 ppm chlorine gas in a sealed chamber for 5 minutes. One hour post-exposure, mice are randomized into vehicle control and treatment groups (n=8/group). Formoterol fumarate dihydrate is dissolved in sterile saline and administered via intraperitoneal injection at 0.3 μg/kg or 1 μg/kg. Airway hyperreactivity to methacholine is measured by whole-body plethysmography 24 hours post-exposure, and lungs are harvested for histopathological analysis [1]
- OVA-sensitized asthma mouse model: Female BALB/c mice (6–8 weeks old) are sensitized with OVA (10 μg) plus aluminum hydroxide adjuvant intraperitoneally on days 0 and 14, then challenged with aerosolized OVA (1% w/v) for 30 minutes on days 21–23. Mice are treated with Formoterol fumarate dihydrate (0.5 μg/kg) dissolved in sterile saline via nebulization once daily for 7 days (days 17–23). Lungs are collected for mRNA extraction (MUC5AC) and histopathological examination [1] |
| Toxicity/Toxicokinetics |
In vivo tolerability: Intraperitoneal injection of up to 1 μg/kg formoterol fumarate dihydrate in mice did not significantly change body weight, food intake, or hematologic/biochemical parameters (ALT, AST, BUN, creatinine) [1]
- Adverse events in children: In the 12-week clinical trial, common treatment-related adverse events included tremor (8.3%), headache (6.7%), and palpitations (3.3%); all events were mild to moderate and resolved spontaneously without discontinuation of the drug [2] |
| References | |
| Additional Infomation |
Formoterol fumarate is the fumarate form of formoterol, a long-acting, selective sympathomimetic β-receptor agonist with bronchodilatory effects. Formoterol fumarate binds to β2-adrenergic receptors in bronchial smooth muscle, stimulating intracellular adenylate cyclase, thereby increasing the production of cyclic adenosine monophosphate (cAMP). Elevated cAMP levels lead to bronchial smooth muscle relaxation, improved mucociliary clearance, and reduced release of mediators from inflammatory cells, particularly mast cells. (NCI05)
A long-duration adrenergic β2-receptor agonist. It is used to treat asthma and chronic obstructive pulmonary disease. See also: Formoterol fumarate (note moved to). Formoterol fumarate dihydrate is a long-acting β₂-adrenergic receptor agonist (LABA) used to treat asthma and chronic obstructive pulmonary disease (COPD)[1][2] - Its mechanism of action involves selectively activating β₂-adrenergic receptors in airway smooth muscle cells, increasing intracellular cAMP levels to induce bronchodilation; it also inhibits airway smooth muscle proliferation and reduces the production of pro-inflammatory chemokines in bronchial epithelial cells[1] - Clinical efficacy in children with asthma: In children aged 6-12 years with mild to moderate asthma, inhalation of formoterol fumarate dihydrate (9 μg, twice daily) improved lung function (FEV₁), reduced asthma symptoms and acute exacerbation rate, and had no serious adverse events[2] - It has a rapid onset of action (within 5 minutes) and a long duration of action (12 hours), making it suitable for maintenance therapy and relief of acute symptoms of asthma[1] - The dosage form is an inhaled aerosol or dry powder inhaler; the recommended dose for children with asthma is 9 μg twice daily (maximum daily dose 18 μg) [2] |
| Molecular Formula |
2(C19H24N2O4).C4H4O4.2(H2O)
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|---|---|
| Molecular Weight |
496.51
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| Exact Mass |
840.379
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| CAS # |
183814-30-4
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| Related CAS # |
Formoterol fumarate; 43229-80-7
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| PubChem CID |
60196271
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| Appearance |
White to off-white solid powder
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| Boiling Point |
603.2ºC at 760 mmHg
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| Melting Point |
116-120ºC
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| Flash Point |
318.6ºC
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| Vapour Pressure |
2.12E-15mmHg at 25°C
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| LogP |
6.229
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
60
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| Complexity |
507
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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.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=C/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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| 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 | 2.0141 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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