| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Tulobuterol Hydrochloride targets the β₂-adrenergic receptor (β₂-AR). It acts as a long-acting agonist, binding to the receptor and stimulating adenylyl cyclase, which increases intracellular cyclic AMP (cAMP) levels. This leads to the relaxation of bronchial smooth muscle, resulting in bronchodilation. The compound has been shown to bind to bovine skeletal muscle β₂-AR with a Kd of 0.13 µM.
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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. Both the quantity and intensity of green fluorescence shown by acidic endosomes in cells were diminished during 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 has been shown to decrease viral RNA levels in human tracheal epithelial cells infected with rhinovirus. This suggests that the compound may have additional antiviral and anti-inflammatory effects beyond bronchodilation. Its ability to inhibit viral replication and modulate airway inflammation could be beneficial in treating respiratory infections that exacerbate asthma and COPD. |
| 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. Consequently, during the 4-hour endotoxin delivery interval using the tuloterol patch, diaphragm contractility was maintained for longer than 24 hours [3].
In vivo, tulobuterol is effective as a bronchodilator, reducing the incidence and severity of bronchial asthma and COPD. The transdermal patch formulation provides sustained drug delivery over 24 hours, maintaining consistent plasma concentrations and improving patient compliance. It has also been shown to increase normal diaphragm muscle strength. |
| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for tulobuterol involve studying its affinity for the β₂-adrenergic receptor. Membrane preparations from cells expressing the receptor are incubated with a radiolabeled antagonist, such as [³H]CGP-12177, in the presence of varying concentrations of tulobuterol. The amount of bound radioactivity is measured to calculate the Ki or IC50, quantifying the compound's affinity for the receptor.
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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. In vitro cell-based assays for tulobuterol are performed using cell lines expressing the β₂-adrenergic receptor, such as human tracheal epithelial cells. Cells are treated with the compound, and the increase in intracellular cAMP levels is measured using ELISA or a cAMP assay kit as a functional readout of receptor activation. Antiviral activity is assessed by infecting cells with rhinovirus and measuring viral RNA levels via qPCR. |
| Animal Protocol |
In vivo animal experiments for tulobuterol are conducted using animal models of asthma and COPD, such as guinea pigs or mice sensitized to an allergen. The compound is administered, and airway resistance is measured to evaluate bronchodilation. In models of viral infection, the compound's ability to reduce viral titers and inflammation in the lungs is assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of tulobuterol Hydrochloride are characterized by its sustained release when administered as a transdermal patch. The compound has a molecular weight of 264.19 and a formula of C₁₂H₁₉Cl₂NO. It is absorbed through the skin, providing a steady-state concentration over 24 hours, which is beneficial for once-daily dosing. The compound is metabolized in the liver and excreted renally.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for tulobuterol Hydrochloride indicate it is generally well-tolerated. Common side effects include local skin reactions at the application site, such as redness and itching. Systemic effects, such as tremor, tachycardia, and hypokalemia, can occur but are less common with the transdermal route due to lower peak plasma concentrations.
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| References | |
| Additional Infomation |
Tulobuterol hydrochloride is an organic molecular entity.
Other information: Tulobuterol Hydrochloride is marketed as a transdermal patch (Hokunalin Tape) in Japan for the treatment of asthma and COPD. It is also available as an oral preparation in some countries. Its long-acting nature and unique delivery system make it a valuable option for patients requiring chronic bronchodilator therapy. |
| Molecular Formula |
C12H19CL2NO
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|---|---|
| Molecular Weight |
264.1914
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| Exact Mass |
263.084
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| CAS # |
56776-01-3
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| Related CAS # |
Tulobuterol;41570-61-0
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| PubChem CID |
5702285
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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 |
163ºC
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| Flash Point |
158.3ºC
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| LogP |
3.954
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
16
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| Complexity |
191
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RSLNRVYIRDVHLY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H18ClNO.ClH/c1-12(2,3)14-8-11(15)9-6-4-5-7-10(9)13;/h4-7,11,14-15H,8H2,1-3H3;1H
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| Chemical Name |
2-(tert-butylamino)-1-(2-chlorophenyl)ethanol;hydrochloride
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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) |
H2O : ~100 mg/mL (~378.52 mM)
DMSO : ~50 mg/mL (~189.26 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.46 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 (9.46 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 (9.46 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: 100 mg/mL (378.52 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 | 3.7852 mL | 18.9258 mL | 37.8515 mL | |
| 5 mM | 0.7570 mL | 3.7852 mL | 7.5703 mL | |
| 10 mM | 0.3785 mL | 1.8926 mL | 3.7852 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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