| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| Other Sizes |
Purity: ≥98%
| Targets |
Not identified in the document.
The primary target of fenoterol hydrochloride is the β2 adrenoreceptor. It acts on beta-2 receptors in the bronchial muscle causing bronchodilation. It also promotes secretion from serous and mucus cells, enhances mucociliary beating, and increases the movement of water and chloride ions into the bronchial lumen. It is a sympathomimetic beta agonist. |
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| ln Vitro |
In a quantitative high-throughput screen (qHTS) using CD63-GFP-expressing C4-2B prostate cancer cells, Fenoterol hydrochloride was identified as an activator of exosome biogenesis and/or secretion, increasing intracellular CD63-GFP signal. Validation by qNano IZON and MACSQuant flow cytometry confirmed that Fenoterol hydrochloride (tested at 10 µM) increased exosome concentration in conditioned media of C4-2B-CD63-GFP cells compared to vehicle-treated controls. [1]
In vitro, fenoterol hydrochloride acts as a potent β2 adrenergic agonist. It binds to β2 adrenoreceptors and activates downstream signaling pathways, leading to smooth muscle relaxation. It promotes secretion from serous and mucus cells and enhances mucociliary beating. These in vitro activities explain its bronchodilatory and tocolytic effects. |
| ln Vivo |
In vivo, fenoterol hydrochloride is used as a bronchodilator for the treatment of asthma and other obstructive airway diseases. It is also used as a tocolytic agent to delay premature labor. It opens up the airways to the lungs. It promotes secretion from serous and mucus cells and enhances mucociliary beating. Its effects are mediated through β2 adrenoreceptor activation.
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| Enzyme Assay |
General protocols for β2 adrenoreceptor binding assays use membrane preparations from cells expressing recombinant human β2 adrenoreceptors (e.g., CHO or HEK293 cells). Membranes are incubated with [3H]CGP-12177 or [125I]iodocyanopindolol and varying concentrations of fenoterol hydrochloride (0.1 nM-100 µM) in binding buffer (50 mM Tris-HCl pH 7.4, 10 mM MgCl2) at 25°C for 60-90 minutes. Nonspecific binding is determined using 10 µM propranolol. Bound ligand is separated by filtration through GF/B filters and counted. Ki values are calculated from competition curves.
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| Cell Assay |
C4-2B-CD63-GFP cells were seeded in 1536-well poly-D-lysine coated plates at 2,000 cells/well in RPMI with 10% serum and 1% Geneticin, incubated for 48 h, then media replaced with serum-free Opti-MEM and 1% Geneticin overnight. Compounds (including Fenoterol hydrochloride at 10 µM) were added via pin-tool (23 nL of DMSO solutions) and incubated for 96 h. GFP fluorescence was quantified using an Acumen laser scanning cytometer. For validation, cells were treated in exosome-free media for 48 h, exosomes isolated by differential ultracentrifugation (300×g 10 min, 20,000×g 30 min, 0.8 µm filtration, 110,000×g 2 h, 100,000×g 1 h), and analyzed by qNano IZON (NP100 nanopore, calibrated with CPC100B and CPC70D beads) and MACSQuant flow cytometry (488 nm excitation, 525/50 nm bandpass, volumetric counting). [1]
General protocols for β2 adrenoreceptor functional assays use cells expressing recombinant β2 receptors coupled to Gs proteins. Cells are seeded in 96-well plates and treated with fenoterol hydrochloride (0.1 nM-100 µM) for 10-30 minutes. cAMP accumulation is measured using a competitive ELISA or HTRF assay. The EC50 is calculated from dose-response curves. Isoproterenol serves as a full agonist control. Bronchial smooth muscle relaxation is assessed using isolated tracheal rings in organ baths. |
| Animal Protocol |
General protocols for in vivo bronchodilator efficacy studies use animal models of bronchoconstriction (e.g., guinea pig or rat models). Bronchoconstriction is induced by histamine, acetylcholine, or antigen challenge. Fenoterol hydrochloride is administered by inhalation or intravenously at doses of 0.1-10 mg/kg. Airway resistance and lung compliance are measured using plethysmography. The compound's ability to reverse bronchoconstriction is evaluated. The duration of action is determined.
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| ADME/Pharmacokinetics |
Fenoterol hydrochloride has a molecular weight of 303.78 g/mol (C17H21NO3·HCl). It is soluble in DMSO but not in water. It is a β2 adrenergic agonist that is administered by inhalation or injection. Following administration, it is rapidly absorbed and distributed to the lungs. It is metabolized in the liver and excreted via the kidneys. The half-life is approximately 2-3 hours. It is a sympathomimetic beta agonist and asthma medication.
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| Toxicity/Toxicokinetics |
Fenoterol hydrochloride has a well-established safety profile. Common adverse effects include tremor, palpitations, tachycardia, headache, and nervousness. High doses may cause hypokalemia, cardiac arrhythmias, and hyperglycemia. It should be used with caution in patients with cardiovascular disease, hypertension, hyperthyroidism, or diabetes. Overdose may require supportive care. The compound is contraindicated in patients with known hypersensitivity.
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| References |
High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8(1):8161.Jozwiak K, Plazinska A, Toll L, Jimenez L, Woo AY, XiaoRP, Wainer IW. Effect of fenoterol stereochemistry on the β2 adrenergic receptor system: ligand-directed chiral recognition. Chirality. 2011;23 Suppl E1-6. doi: 10.1002/chir.20963. Epub 2011 May 26. Review. PubMed PMID: 21618615; PubMed Central PMCID: PMC3164500.
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| Additional Infomation |
See also: Fenoterol Hydrochloride (note moved to).
Fenoterol hydrochloride was identified as one of 22 confirmed hits from a qHTS of the LOPAC and NPC libraries that modulate exosome biogenesis/secretion. It was validated as an activator of exosome production in prostate cancer cells, increasing exosome concentration in cell supernatants. The study suggests exosome biogenesis activators may have therapeutic implications in immunoregulation, though specific mechanisms for Fenoterol hydrochloride were not elucidated. [1] Fenoterol hydrochloride (CAS 1944-10-1) is a potent β2 adrenergic agonist used as a bronchodilator for asthma and other obstructive airway diseases. It is also used as a tocolytic agent. It is approved by the FDA, EMA, and other regulatory agencies for these indications. It is available in various formulations, including metered-dose inhalers, nebulizer solutions, and oral tablets. It is an essential medicine in respiratory care. |
| Molecular Formula |
C17H22CLNO4
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|---|---|
| Molecular Weight |
303.353
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| Exact Mass |
339.124
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| CAS # |
1944-10-1
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| Related CAS # |
1944-10-1 (HCl);1944-12-3 (HBr);13392-18-2;130156-24-0 (RS isomer); 36369-23-0 (RS isomer HBr); 130156-24-0 (RS isomer);
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| PubChem CID |
21981128
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.25
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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 |
OC1=CC=C(CC(NCC(C2=CC(O)=CC(O)=C2)O)C)C=C1
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| InChi Key |
HNINVRLEFUPHLU-NRNQBQMASA-N
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| InChi Code |
InChI=1S/C17H21NO4.ClH/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,6,10H2,1H31H/t11-,17+/m1./s1
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| Chemical Name |
(1RS)-1-(3,5-Dihydroxyphenyl)-2-(((1RS)-2-(4-hydroxyphenyl)-1-methylethyl)amino)ethanol hydrochloride
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| Synonyms |
Th-1165a Th1165aTh 1165aPhenoterol hydrobromide, Berotec, p Hydroxyphenylorciprenaline, Partusisten, Phenoterol Fenoterol HCl TH-1179
hydrochloride UNII-3DM11M5URG NSC-292265.
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.2965 mL | 16.4826 mL | 32.9652 mL | |
| 5 mM | 0.6593 mL | 3.2965 mL | 6.5930 mL | |
| 10 mM | 0.3297 mL | 1.6483 mL | 3.2965 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 |
| NCT02177370 | TERMINATED | Drug: Fenoterol MDI Drug: DSCG MDI |
Asthma | Boehringer Ingelheim | 1990-02 | Phase 3 |
| NCT01440335 | COMPLETED | Drug: Oral R,R'-Fenoterol Drug: Oral Racemic Fenoterol |
Congestive Heart Failure | National Institute on Aging (NIA) | 2011-07-10 | Phase 1 |
| NCT02182479 | COMPLETED | Drug: Berodual® via Respimat®, high dose Drug: Berodual® via Respimat®, low dose Drug: Berodual® via MDI, high dose |
Asthma | Boehringer Ingelheim | 1998-04 | Phase 3 |
| NCT02173782 | COMPLETED | Drug: Berodual® Respimat ® high dose
Drug: Berodual® Respimat ® low dose Drug: Berodual® MDI Drug: Placebo |
Pulmonary Disease, Chronic Obstructive | Boehringer Ingelheim | 1998-02 | Phase 3 |
| NCT00460577 | COMPLETEDWITH RESULTS | Drug: Formoterol fumerate Drug: fenoterol/ipratropium bromide |
Acute Bronchial Obstruction, Asthma | Novartis | 2007-03 | Phase 4 |
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