| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
β2 adrenoreceptor
Fenoterol hydrobromide targets the β2-adrenergic receptor, a G protein-coupled receptor expressed primarily on bronchial smooth muscle cells. As a selective agonist, fenoterol activates β2-adrenergic receptors, leading to the activation of adenylate cyclase and an increase in intracellular cAMP levels. This results in relaxation of bronchial smooth muscle, bronchodilation, and relief of bronchospasm. Fenoterol also has tocolytic (uterine relaxant) effects. |
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| 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 studies demonstrate that fenoterol hydrobromide acts as a selective β2-adrenergic receptor agonist. Its activity can be assessed using cell-based assays in which cells expressing the β2-adrenergic receptor are treated with the compound and the resulting increase in cAMP accumulation is measured using a cAMP ELISA or HTRF-based assay. The EC50 for receptor activation is determined from dose-response curves. |
| ln Vivo |
Fenoterol hydrobromide (0.7 mg/kg; intraperitoneal injection; twice a day; for 3 weeks) suppresses mechanical allodynia during chronic treatment[3].
Fenoterol hydrobromide is used in vivo as a bronchodilator for the treatment of asthma, COPD, and other respiratory conditions. It is available in various formulations, including metered-dose inhalers and nebulizer solutions. The compound's bronchodilator effects are rapid in onset and provide relief from bronchospasm. Fenoterol is also used as a tocolytic agent to delay premature labor. |
| Enzyme Assay |
Non-cellular receptor binding assays for fenoterol hydrobromide involve competitive radioligand binding displacement studies using membrane preparations from cells expressing the human β2-adrenergic receptor. The membranes are incubated with a radiolabeled β2-selective ligand (e.g., [³H]CGP-12177) and varying concentrations of fenoterol. Following incubation and filtration, the radioactivity is measured to determine the IC50, which is then converted to a Ki value using the Cheng-Prusoff equation.
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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 hydrobromide involve treating cells expressing the β2-adrenergic receptor with the compound and measuring receptor-mediated signaling. Cells are treated with varying concentrations of fenoterol, and the activation of the receptor is measured by quantifying cAMP accumulation using a cAMP ELISA or HTRF-based assay. The EC50 for receptor activation is determined from dose-response curves. The compound's selectivity for β2 over β1 receptors can be assessed using parallel assays with cells expressing β1 receptors. |
| 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 with fenoterol hydrobromide are conducted in animal models of bronchoconstriction. Guinea pigs or rats are exposed to bronchoconstrictive agents (e.g., histamine or methacholine) and treated with fenoterol via inhalation or intravenous administration. The compound's ability to reverse bronchoconstriction is assessed by measuring airway resistance or lung function parameters. Tocolysis studies are conducted in pregnant animal models. |
| ADME/Pharmacokinetics |
Fenoterol hydrobromide has a molecular weight of 384.26 and a molecular formula of C17H22BrNO4. It is a white crystalline powder with a purity of ≥98%. The compound is soluble in water and other polar solvents. It is typically stored at room temperature in a dry place, protected from light. Pharmacokinetic studies show that fenoterol is rapidly absorbed after inhalation and has a relatively short duration of action, requiring frequent dosing for sustained bronchodilation.
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| Toxicity/Toxicokinetics |
Fenoterol hydrobromide is generally well-tolerated at therapeutic doses. Common side effects include tremor, palpitations, headache, and tachycardia, which are related to β2-adrenergic receptor stimulation. At high doses, fenoterol may cause hypokalemia and cardiac arrhythmias. The compound should be used with caution in patients with cardiovascular disease, hypertension, or hyperthyroidism.
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| References |
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| Additional Infomation |
Fenoterol hydrobromide is the hydrobromide salt of fenoterol. It is a β2-adrenergic agonist used to treat reversible airway obstruction and is a bronchodilator. It has bronchodilatory, β-adrenergic agonist, and sympathomimetic effects. It contains fenoterol. Fenoterol hydrobromide is a short-acting sympathomimetic agent with bronchodilatory effects. Fenoterol stimulates β2-adrenergic receptors in the lungs, thereby activating adenylate cyclase, which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP). Increased cAMP concentration relaxes bronchial smooth muscle, relieves bronchospasm, and reduces the release of inflammatory cytokines, especially those from mast cells. A synthetic β2-adrenergic agonist used as a bronchodilator and uterine contraction inhibitor.
Fenoterol hydrobromide (CAS 1944-12-3) is a selective, orally active β2-adrenergic receptor agonist used as a bronchodilator for the treatment of asthma, COPD, and other respiratory conditions. It is also used as a tocolytic agent. The compound's mechanism of action involves activation of β2-adrenergic receptors on bronchial smooth muscle, leading to bronchodilation. Fenoterol hydrobromide is available from various pharmaceutical suppliers for research and clinical applications. |
| Molecular Formula |
C17H22BRNO4
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|---|---|
| Molecular Weight |
384.26488
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| Exact Mass |
383.073
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| Elemental Analysis |
C, 53.14; H, 5.77; Br, 20.79; N, 3.65; O, 16.65
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| CAS # |
1944-12-3
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| Related CAS # |
Fenoterol; 13392-18-2; Fenoterol-d6 hydrobromide; 1286129-04-1
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| PubChem CID |
5702161
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| Appearance |
White to off-white solid powder
|
| Melting Point |
226-228°C
|
| Vapour Pressure |
1.19E-13mmHg at 25°C
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| LogP |
3.406
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
23
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| Complexity |
310
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(CC1=CC=C(C=C1)O)NCC(C2=CC(=CC(=C2)O)O)O.Br
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| InChi Key |
SGZRQMALQBXAIQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H21NO4.BrH/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;1H
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| Chemical Name |
5-[1-hydroxy-2-[1-(4-hydroxyphenyl)propan-2-ylamino]ethyl]benzene-1,3-diol;hydrobromide
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| Synonyms |
Fenoterol hydrobromide; Fenoterol HBr; Phenoterol hydrobromide; TH 1165A; TH-1165A; TH1165A; Berotec hydroxyphenylorciprenaline
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~260.2 mM)
H2O: ~25 mg/mL (~65.1 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.51 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 (6.51 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 60 mg/mL (156.14 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6024 mL | 13.0120 mL | 26.0240 mL | |
| 5 mM | 0.5205 mL | 2.6024 mL | 5.2048 mL | |
| 10 mM | 0.2602 mL | 1.3012 mL | 2.6024 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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