| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
β2-adrenergic receptor (β2-AR). Tulobuterol selectively binds to and activates β2-adrenoceptors on bronchial airway smooth muscle cells.
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| ln Vitro |
At one and three days postinfection, tulobuterol (0.1 μM; 24 h or 72 h; human tracheal epithelial cells) therapy decreased RV14 RNA levels. Prior to RV14 infection, the supernatants of cells treated with tulobutero had a considerably lower concentration of sICAM-1 than did the cells treated with vehicle. The quantity and intensity of green-fluorescent acidic endosomes in cells were both decreased by tulobuterol treatment. also decreased the release of IL-1β, IL-6, and IL-8 brought on by RV14 infection. RV14-induced NF-κB p50, p65, and c-Rel levels were significantly but modestly reduced upon tulobuterol administration [1].
In vitro, Tulobuterol (0.1 μM) activates β2-adrenoceptors, stimulating adenylate cyclase activity and increasing intracellular cAMP levels. Elevated cAMP activates protein kinase A (PKA), which phosphorylates various proteins involved in smooth muscle relaxation, including myosin light chain kinase (MLCK) and calcium channels, leading to bronchodilation. |
| ln Vivo |
The study investigated the impact of tuloterol on the contractility of diaphragms extracted from endotoxin-treated mice (BALBs/c animals; 21.7 ± 0.2 g). With the use of force-frequency curves of untreated or treated diaphragms at 0 (E0) and 4 (E4) hours following the administration of an E. Coli endotoxin (20 mg/kg), contractile characteristics and twitch kinetics were determined. After transdermal tuloterol treatment, E0 and E4 diaphragms were examined 0, 12, and 24 hours later. The tuloterol patch restored muscular contractility, as evidenced by the force-frequency curves of the E0 and E4 diaphragms at the three time periods that did not significantly differ from one another. Thus, during the 4-hour endotoxin treatment interval, diaphragm contractility was sustained for over 24 hours with the use of the tuloterol patch [2].
In vivo, Tulobuterol has been studied in preclinical models of asthma and COPD, demonstrating bronchodilatory effects through reduced airway resistance and improved airflow. It reduces the frequency of exacerbations of chronic obstructive pulmonary disease. |
| Enzyme Assay |
Typical non-cell receptor binding assays for β2-AR agonists involve radioligand competition binding using membrane preparations from cells overexpressing human β2-AR. Membranes are incubated with a fixed concentration of a radiolabeled antagonist (e.g., [³H]-dihydroalprenolol) and varying concentrations of Tulobuterol. Nonspecific binding is determined in the presence of excess propranolol. After incubation, bound and free ligand are separated by filtration through glass fiber filters, and radioactivity is measured by scintillation counting to calculate IC50 and Ki values.
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| Cell Assay |
RT-PCR[1]
Cell Types: Human tracheal epithelial cells infected with RV14 Tested Concentrations: 0.1 μM Incubation Duration: 24 hrs (hours) or 72 hrs (hours) Experimental Results: RV14 RNA levels diminished 1 and 3 days after infection. The concentration of sICAM-1 in the cell supernatant was Dramatically diminished. Reduce the number of intracellular green fluorescent acidic endosomes and the fluorescence intensity of intracellular acidic endosomes. The secretion of IL-1β, IL-6, and IL-8 induced by RV14 infection was also diminished. RV14 infection induced a small but significant reduction in the amounts of p50, p65, and c-Rel of NF-κB. Cellular assays are performed using cell lines (e.g., CHO or HEK-293) stably expressing human β2-AR. Cells are seeded in multi-well plates and treated with varying concentrations of Tulobuterol. The functional response is measured by quantifying intracellular cAMP accumulation using a competitive ELISA or homogeneous time-resolved fluorescence (HTRF) assay. Cells are lysed after treatment, and cAMP levels are determined against a standard curve. EC50 values are calculated from dose-response curves. |
| Animal Protocol |
Animal studies are conducted in rodent models of airway hyperresponsiveness, such as ovalbumin-sensitized and challenged mice or guinea pigs. Tulobuterol is administered via oral gavage, inhalation, or transdermal application at doses ranging from 0.1 to 10 mg/kg. Airway resistance and dynamic compliance are measured using whole-body plethysmography or invasive pulmonary mechanics. Bronchoalveolar lavage fluid is collected to assess inflammatory cell infiltration and cytokine levels.
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| ADME/Pharmacokinetics |
Tulobuterol is absorbed rapidly after oral administration and undergoes extensive first-pass metabolism. The transdermal patch formulation provides sustained drug delivery over 24 hours. The compound is primarily metabolized in the liver and excreted in urine. Plasma protein binding is moderate. The elimination half-life is approximately 3-5 hours for oral formulations and extended with transdermal delivery.
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| Toxicity/Toxicokinetics |
In preclinical toxicology studies, Tulobuterol shows a favorable safety profile at therapeutic doses. Common adverse effects at supratherapeutic doses include tachycardia, tremor, and hypokalemia, consistent with β2-agonist pharmacology. No significant genotoxicity or carcinogenicity has been reported in standard assays. The compound is not recommended for use during pregnancy without careful risk-benefit assessment.
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| References | |
| Additional Infomation |
2-(tert-butylamino)-1-(2-chlorophenyl)ethanol is an organochlorine compound. Tobacterol has been used in clinical trials for the treatment of chronic obstructive pulmonary disease. Indications: Paroxysmal wheezing, asthma.
Tulobuterol is a β2-adrenoceptor agonist that induces bronchodilation through the cAMP/PKA signaling pathway. Clinical trials have evaluated its efficacy in asthma and COPD, showing improved lung function and reduced symptom scores. It is approved in several countries for the treatment of asthma and COPD, available as oral tablets and transdermal patches. The transdermal formulation offers the advantage of once-daily application and reduced systemic side effects. |
| Molecular Formula |
C12H18CLNO
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|---|---|
| Molecular Weight |
227.7304
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| Exact Mass |
227.108
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| CAS # |
41570-61-0
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| Related CAS # |
Tulobuterol-d9 hydrochloride;1325559-14-5;Tulobuterol hydrochloride;56776-01-3
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| PubChem CID |
5606
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| Appearance |
White to off-white solid powder
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| Density |
1.098 g/cm3
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| Boiling Point |
338.2ºC at 760 mmHg
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| Melting Point |
89-91ºC
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| Flash Point |
158.3ºC
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| LogP |
3.152
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
15
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| Complexity |
191
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YREYLAVBNPACJM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H18ClNO/c1-12(2,3)14-8-11(15)9-6-4-5-7-10(9)13/h4-7,11,14-15H,8H2,1-3H3
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| Chemical Name |
2-(tert-butylamino)-1-(2-chlorophenyl)ethanol
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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 (~439.12 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.98 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 (10.98 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 (10.98 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3912 mL | 21.9558 mL | 43.9116 mL | |
| 5 mM | 0.8782 mL | 4.3912 mL | 8.7823 mL | |
| 10 mM | 0.4391 mL | 2.1956 mL | 4.3912 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.
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