Tulobuterol
(Synonyms: 妥布特罗,C-78 free base) 目录号 : GC62650
A long-acting β2-AR agonist
Cas No.:41570-61-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Tulobuterol is a long-acting agonist of the β2-adrenergic receptor (β2-AR).1 It binds to the bovine skeletal muscle β2-AR (Kd = 0.13 ?M). Transdermal administration of tulobuterol (6 and 12 mg/kg) decreases total leukocyte infiltration into the bronchoalveolar lavage fluid (BALF) in a mouse model of allergic asthma induced by ovalbumin.2 It also inhibits rhinovirus replication in infected primary human tracheal epithelial cells when used at a concentration of 0.1 ?M, an effect that can be reversed by the β2-AR antagonist ICI 118551 .3 Formulations containing tulobuterol have been used in the treatment of asthma.
1.IJzerman, A.P., Bultsma, T., and Timmerman, H.Quantitative evaluation of the β2-adrenoceptor intrinsic activity of N-tert-butylphenylethanolaminesJ. Med. Chem.29(4)549-554(1986) 2.Fu, L., Guan, J., Zhang, Y., et al.Tulobuterol patch alleviates allergic asthmic inflammation by blockade of Syk and NF-κB activation in miceOncotarget9(15)12154-12163(2018) 3.Yamaya, M., Nishimura, H., Nadine, L., et al.Tulobuterol inhibits rhinovirus infection in primary cultures of human tracheal epithelial cellsPhysiol. Rep.1(3)e00041(2013)
| Cas No. | 41570-61-0 | SDF | |
| 别名 | 妥布特罗,C-78 free base | ||
| 分子式 | C12H18ClNO | 分子量 | 227.73 |
| 溶解度 | DMSO : 100 mg/mL (439.12 mM; Need ultrasonic) | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Transdermal Tulobuterol patch, a long-actingβ(2)-agonist
Allergol Int 2012 Jun;61(2):219-29.PMID:22270072DOI:10.2332/allergolint.11-RA-0358.
Tulobuterol patch (HokunalinTM Tape), which contains a β(2)-adrenergic agonist, is the first bronchodilator to be available as a transdermal patch. This drug delivery system ensures that the time at which the peak drug concentration in the blood is reached coincides with the morning dip in respiratory function. The use of the patch also prevents excessive increase in blood drug concentrations, thereby reducing the incidence of systemic adverse reactions. Since 1998, when it was first approved in Japan and worldwide, the Tulobuterol patch has been used widely in the treatment of bronchial asthma and chronic obstructive pulmonary disease (COPD), and evidence collected since it was approved has confirmed its clinical efficacy and safety. Because the patch is easy to use and requires only once-daily application, treatment adherence of patients using the patch is good. In this article, we discuss the rationale behind the development of the Tulobuterol patch, evaluate data on its clinical efficacy and safety in the treatment of asthma and COPD, and examine the treatment adherence in individuals using the patch.
Skin permeability of Tulobuterol in two transdermal formulations and their followability
Drug Discov Ther 2017 Nov 22;11(5):253-258.PMID:29021505DOI:10.5582/ddt.2017.01050.
Various generic transdermal formulations of Tulobuterol containing rubber and acrylate base polymers are commercially available in Japan. However, none of the formulations have been compared directly with respect to the skin permeability of Tulobuterol and to their follow ability. Tulobuterol Tape Sawai of rubber base and Tulobuterol Tape NP of acrylate base were used to conduct the in vitro 24-hour skin permeability test of Tulobuterol at receiver solution temperatures of 32°C, 37°C, and 40°C. Furthermore, the followability of these tapes were examined by measuring the depth of the pores that were formed in their adhesive layer. Consequently, the maximum flux of Tulobuterol was greater for Tulobuterol Tape NP. Arrhenius plot analysis revealed that Tulobuterol Tape Sawai was more sensitive to skin surface temperature compared with Tulobuterol Tape NP. Skin abrasion had a greater effect on the skin permeability of Tulobuterol in Tulobuterol Tape Sawai than in Tulobuterol Tape NP. Followability was greater for Tulobuterol Tape NP than for Tulobuterol Tape Sawai. These results suggest that a transdermal formulation of acrylate base is preferable to that with a rubber base when skin surface temperature varies or when the skin is abraded. In clinical settings, therefore, a formulation of acrylate base is preferable to a formulation of rubber base when skin surface temperature varies or when the skin is abraded. The formulation needs to be applied to the skin of less asperity for the achievement of better transdermal absorption of Tulobuterol.
Sustained release of Tulobuterol from graphene oxide laden hydrogel to manage asthma
J Biomater Sci Polym Ed 2021 Mar;32(4):524-535.PMID:33175639DOI:10.1080/09205063.2020.1849921.
Bronchial asthma is a chronic disease which is currently treated using various inhalants. However, the medication adherence with the inhalants is poor due to complex procedure to use them along with frequent dosing. In this paper, we have developed Tulobuterol loaded Pluronic® F127-reduced graphene oxide transdermal hydrogel to sustain the release of Tulobuterol to manage asthma for days. The synthesis of Pluronic® F127-reduced graphene oxide was confirmed by Fourier transform infrared spectroscopy, X-ray diffraction, and Raman spectroscopy. The transmission electron microscope showed wrinkled flat nano sheets. The hydrogel showed sufficient mechanical properties for topical application and was safe in the skin irritation study (rabbit model). The ex vivo release data demonstrated the ability of reduced graphene oxide to sustain the release of Tulobuterol for 72 h, due to strong π-π interaction between drug and graphene oxide. The pharmacokinetic profile in Sprague-Dawley rat model confirmed the potential of tulobuterol-Pluronic® F127-reduced graphene oxide hydrogel to sustain the release of Tulobuterol for effective management of asthma.
Tulobuterol patch alleviates allergic asthmic inflammation by blockade of Syk and NF-κB activation in mice
Oncotarget 2018 Jan 31;9(15):12154-12163.PMID:29552299DOI:10.18632/oncotarget.24348.
Background: Tulobuterol patch, one of strongest bronchodilators, was recently shown to improve bronchial hyperresponsiveness and significantly decrease the sputum eosinophil counts by combining with nonspecific anti-inflammatory drugs on patients with asthma. However, there is limited study on the anti-inflammatory activities of Tulobuterol patch and its potential machenism. Results: The Tulobuterol patch significantly ameliorated inflammatory cell infiltration in the lung tissue, reduced the number of total leukocytes and its differential count, markedly reduced the production of IL-1β, TNF-α, IL-6, CCL-11 and IL-4 in bronchial alveolar lavage fluid, as well as a reduction in IL-4/IFN-γ ratio. Tulobuterol patch exhibited the best effect on allergic inflammation compared with formoterol and salbutamol. Furthermore, Tulobuterol patch treatment significantly suppressed the expression and activation of Syk and its downdream signaling NF-κB and p-NF-κB. Conclusions: The present studies revealed that Tulobuterol patch effectively ameliorated airway inflammatory responses in allergic asthma, and its mechanisms, at least partially, via down-regulating Syk/NF-κB pathway. Methods: An ovalbumin induced allergic asthma mouse model were used, and the effects of Tulobuterol patch on allergic airway inflammation were evaluated. Also, its anti-airway inflammatory potential was compared with two other β2-agonists, salbutamol and formoterol. Its possible anti-inflammatory mechanisms were identified by using western blotting and immunohistochemistry.
Tulobuterol inhibits rhinovirus infection in primary cultures of human tracheal epithelial cells
Physiol Rep 2013 Aug;1(3):e00041.PMID:24303127DOI:10.1002/phy2.41.
A transdermal patch preparation of the β2 agonist Tulobuterol has been designed to yield sustained β2 agonistic effects and has been used as a long-acting β2 agonist (LABA) in Japan. LABAs reduce the frequency of exacerbations of chronic obstructive pulmonary disease and bronchial asthma. However, inhibitory effects of LABAs on the replication of rhinovirus (RV), the major cause of exacerbations, have not been demonstrated. To examine the effects of Tulobuterol on RV replication and on the production of the replication-induced pro-inflammatory cytokines, human tracheal epithelial cells were infected with a major group RV, type 14 rhinovirus (RV14). Tulobuterol reduced the RV14 titers and RNA levels; the concentrations of cytokines, including interleukin (IL)-1β, IL-6, and IL-8, in the supernatants; and susceptibility to RV14 infection. Tulobuterol reduced the expression of intercellular adhesion molecule-1 (ICAM-1), the receptor for RV14, and the number of acidic endosomes in the cells in which RV14 RNA enters the cytoplasm. Tulobuterol inhibited the activation of nuclear factor kappa B (NF-κB) proteins in nuclear extracts. A selective β2-adrenergic receptor antagonist, ICI 118551 [erythro-dl-1-(7-methylindan-4-yloxy)-3-isopropylaminobutan-2-ol], reversed the inhibitory effects of Tulobuterol on the RV14 titers and RNA levels, the susceptibility to RV14 infection, cytokine production, and ICAM-1 expression. Tulobuterol may inhibit RV replication by reducing ICAM-1 expression and acidic endosomes and modulate airway inflammation during RV replication.