| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
β2 adrenoreceptor
Fenoterol targets the β2-adrenergic receptor (β2-adrenoceptor). It acts as a selective agonist at this receptor, activating it to cause bronchodilation. Activation of β2-adrenergic receptors on airway smooth muscle cells leads to relaxation and opening of the airways. The compound is classed as a sympathomimetic beta agonist. |
|---|---|
| ln Vitro |
Fenoterol (1 μM; pre-incubated 30 minutes) treatment significantly downregulates the elevated phosphorylation levels of AMPK and reduces AICAR-induced NF-κB activation, TNF-α release, and AMPK activation[2].
Fenoterol suppresses the production of inflammatory cytokines and AMPK activation caused by lipopolysaccharide (LPS) in THP-1 cells[2]. Fenoterol is also a strong inducer of exosome biogenesis and/or secretion in PC cells[4]. In vitro, Fenoterol acts as a selective agonist at the β2-adrenoceptor, activating the receptor and stimulating adenylate cyclase activity. This leads to increased intracellular cAMP levels, which causes smooth muscle relaxation. The compound demonstrates potent bronchodilatory activity in isolated airway preparations. |
| ln Vivo |
Fenoterol (0.7 mg/kg; intraperitoneal injection; twice a day; for 3 weeks) suppresses mechanical allodynia during chronic treatment[3].
In vivo, Fenoterol is an effective bronchodilator used for the treatment of bronchospasm associated with asthma, bronchitis, and other obstructive airway diseases. It is administered orally or via inhalation. Fenoterol is also used as a tocolytic agent to delay premature labor by relaxing uterine smooth muscle. The compound opens up the airways to the lungs. |
| Enzyme Assay |
The in vitro receptor binding assay for Fenoterol involves measuring its affinity for the β2-adrenergic receptor. Radiolabeled ligand binding assays (e.g., using [³H]-dihydroalprenolol) are performed using membrane preparations from cells expressing β2-adrenoceptors. Varying concentrations of Fenoterol are incubated with the receptor preparation, and binding affinity (IC50 or Ki) is determined. Fenoterol acts as a selective β2-adrenoceptor agonist.
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| Cell Assay |
Cell Line: THP-1 cells stimulated with AICAR
Concentration: 1 μM Incubation Time: Pre-incubated 30 minutes Result: Significantly downregulated the elevated phosphorylation levels of AMPK. In vitro cellular assays for Fenoterol involve treating cultured cells expressing β2-adrenergic receptors (e.g., airway smooth muscle cells) with varying concentrations of the compound. cAMP levels are measured using ELISA or radioimmunoassay to assess receptor activation. Smooth muscle cell relaxation is assessed using contractility assays. The compound's potency as a β2-agonist is determined from dose-response curves. |
| Animal Protocol |
Male C57BL/6J mice (6 weeks old) with neuropathy
0.7 mg/kg Intraperitoneal injection; twice a day; for 3 weeks In vivo animal experiments for Fenoterol typically use guinea pig or rat models of bronchoconstriction. Bronchospasm is induced using histamine, acetylcholine, or allergen challenge. Fenoterol is administered via inhalation, oral, or intravenous routes at various doses. Airway resistance and lung function parameters are measured using whole-body plethysmography. The bronchodilatory effect is assessed by measuring the reversal of bronchoconstriction. |
| ADME/Pharmacokinetics |
Metabolism/Metabolites
Liver. Fenoterol is an orally active β2-adrenoceptor agonist. It is administered orally or via inhalation for bronchodilation. The compound has a molecular weight of 303.35 (C17H21NO4). As a small molecule, Fenoterol is expected to be well-absorbed, extensively metabolized in the liver, and excreted via renal and biliary routes. Specific PK parameters (e.g., half-life, bioavailability) are available from clinical pharmacology studies. |
| Toxicity/Toxicokinetics |
Fenoterol is an approved medication for the treatment of asthma and obstructive airway diseases. Common adverse effects associated with β2-agonists include tachycardia, palpitations, tremor, headache, and hypokalemia. The compound is contraindicated in patients with hypertrophic obstructive cardiomyopathy or tachyarrhythmias. As a tocolytic, it may cause maternal and fetal tachycardia and hyperglycemia.
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| References |
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| Additional Infomation |
Fenoterol belongs to the resorcinol class of compounds. Its chemical name is 5-(1-hydroxyethyl)benzene-1,3-diol, in which one methyl hydrogen atom is replaced by 1-(4-hydroxyphenyl)prop-2-amino. It is a β2-adrenergic agonist, used as a bronchodilator in the form of hydrobromide for the treatment of reversible airway obstruction. It has multiple effects as a bronchodilator, sympathomimetic agent, β-adrenergic agonist, and tocolytic. It is a secondary amino compound, a secondary alcohol, and also a resorcinol. Fenoterol is a β2-adrenergic agonist that can be used as a bronchodilator and tocolytic. Fenoterol is a short-acting sympathomimetic agent with bronchodilatory effects. Fenoterol stimulates β2-adrenergic receptors in the lungs, thereby activating adenylate cyclase, an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP). Increased cAMP levels can relax bronchial smooth muscle, relieve bronchospasm, and reduce the release of inflammatory cytokines, especially those from mast cells. Fennoterol is a synthetic β2-adrenergic agonist used as a bronchodilator and a tocolytic. Drug Indications: Fennoterol is used to treat asthma. Mechanism of Action: Pulmonary β2-receptor agonists cause bronchial smooth muscle relaxation, bronchodilation, and increased bronchial airflow. Pharmacodynamics: Fennoterol is a β-receptor agonist designed to open lung airways by reducing bronchial constriction.
Fenoterol (CAS#: 13392-18-2) is a selective, orally active β2-adrenoceptor agonist used as a bronchodilator for asthma, bronchitis, and other obstructive airway diseases. It is also known as Th-1165a and Phenoterol hydrobromide. Fenoterol is clinically approved and marketed in various countries for respiratory indications. It is also used as a tocolytic agent to delay premature labor. |
| Molecular Formula |
C17H21NO4
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|---|---|
| Molecular Weight |
303.36
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| Exact Mass |
303.147
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| Elemental Analysis |
C, 67.31; H, 6.98; N, 4.62; O, 21.10
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| CAS # |
13392-18-2
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| Related CAS # |
Fenoterol hydrobromide; 1944-12-3
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| PubChem CID |
3343
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| Appearance |
Light brown to brown solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
566.0±45.0 °C at 760 mmHg
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| Melting Point |
181-183ºC
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| Flash Point |
203.1±19.3 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.642
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| LogP |
0.89
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| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
22
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| Complexity |
310
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC1=CC(C(O)CNC(C)CC2=CC=C(O)C=C2)=CC(O)=C1
|
| InChi Key |
LSLYOANBFKQKPT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H21NO4/c1-11(6-12-2-4-14(19)5-3-12)18-10-17(22)13-7-15(20)9-16(21)8-13/h2-5,7-9,11,17-22H,6,10H2,1H3
|
| Chemical Name |
5-[1-hydroxy-2-[1-(4-hydroxyphenyl)propan-2-ylamino]ethyl]benzene-1,3-diol
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| Synonyms |
Phenoterol hydrobromide; Berotec; p Hydroxyphenylorciprenaline; Partusisten; Phenoterol; Th-1165a; Th1165a; Th 1165a
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO: ~100 mg/mL (~329.7 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.24 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2964 mL | 16.4821 mL | 32.9641 mL | |
| 5 mM | 0.6593 mL | 3.2964 mL | 6.5928 mL | |
| 10 mM | 0.3296 mL | 1.6482 mL | 3.2964 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 |
| NCT01440335 | Completed | Drug: Oral R,R'-Fenoterol Drug: Oral Racemic Fenoterol |
Congestive Heart Failure | National Institute on Aging (NIA) |
July 10, 2011 | Phase 1 |
| NCT01440335 | Completed | Drug: Oral R,R'-Fenoterol Drug: Oral Racemic Fenoterol |
Congestive Heart Failure | National Institute on Aging (NIA) |
July 10, 2011 | Phase 1 |
| NCT00274066 | Completed | Drug: Tiotropium + placebo Drug: Tiotropium + fenoterol |
Pulmonary Disease, Chronic Obstructive |
Boehringer Ingelheim | October 2002 | Phase 3 |
| NCT05294965 | Completed | Drug: Fenoterol Drug: Mild cold exposure |
Thermogenesis | University Hospital, Basel, Switzerland |
April 27, 2022 | Early Phase 1 |
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