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| 10mg |
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| 25mg |
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Purity: ≥98%
Fenoterol (Th-1165a; Phenoterol hydrobromide), a potent β2 adrenergic agonist designed to open up the airways to the lungs, is classed as sympathomimetic beta agonist and asthma medication.
| Targets |
β2 adrenoreceptor
|
|---|---|
| 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]. |
| ln Vivo |
Fenoterol (0.7 mg/kg; intraperitoneal injection; twice a day; for 3 weeks) suppresses mechanical allodynia during chronic treatment[3].
|
| 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. |
| Animal Protocol |
Male C57BL/6J mice (6 weeks old) with neuropathy
0.7 mg/kg Intraperitoneal injection; twice a day; for 3 weeks |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Hepatic. |
| References |
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| Additional Infomation |
Fenoterol is a member of the class resorcinols that is 5-(1-hydroxyethyl)benzene-1,3-diol in which one of the methyl hydrogens is replaced by a 1-(4-hydroxyphenyl)propan-2-amino group. A beta2-adrenergic agonist, it is used (as the hydrobromide salt) as a bronchodilator in the management of reversible airway obstruction. It has a role as a bronchodilator agent, a sympathomimetic agent, a beta-adrenergic agonist and a tocolytic agent. It is a secondary amino compound, a secondary alcohol and a member of resorcinols.
Fenoterol is an adrenergic beta-2 agonist that is used as a bronchodilator and tocolytic. Fenoterol is a short-acting sympathomimetic agent with bronchodilator activity. Fenoterol stimulates beta-2-adrenergic receptors in the lungs, thereby activating the enzyme adenylate cyclase that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased cAMP concentrations relax bronchial smooth muscle, relieve bronchospasms, and reduce inflammatory cell mediator release, especially from mast cells. A synthetic adrenergic beta-2 agonist that is used as a bronchodilator and tocolytic. Drug Indication Fenoterol is used for the treatment of asthma. Mechanism of Action Beta(2)-receptor stimulation in the lung causes relaxation of bronchial smooth muscle, bronchodilation, and increased bronchial airflow. Pharmacodynamics Fenoterol is a beta agonist designed to open up the airways to the lungs by decreasing bronchconstriction. |
| Molecular Formula |
C17H21NO4
|
|---|---|
| Molecular Weight |
303.36
|
| Exact Mass |
303.147
|
| Elemental Analysis |
C, 67.31; H, 6.98; N, 4.62; O, 21.10
|
| CAS # |
13392-18-2
|
| Related CAS # |
Fenoterol hydrobromide; 1944-12-3
|
| PubChem CID |
3343
|
| Appearance |
Light brown to brown solid powder
|
| Density |
1.3±0.1 g/cm3
|
| 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
|
| Vapour Pressure |
0.0±1.6 mmHg at 25°C
|
| Index of Refraction |
1.642
|
| LogP |
0.89
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
22
|
| Complexity |
310
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
OC1=CC(C(O)CNC(C)CC2=CC=C(O)C=C2)=CC(O)=C1
|
| InChi Key |
LSLYOANBFKQKPT-UHFFFAOYSA-N
|
| 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
|
| Synonyms |
Phenoterol hydrobromide; Berotec; p Hydroxyphenylorciprenaline; Partusisten; Phenoterol; Th-1165a; Th1165a; Th 1165a
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~329.7 mM)
|
|---|---|
| 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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