Salmeterol xinafoate
(Synonyms: 沙美特罗昔萘酸酯; GR 33343X xinafoate) 目录号 : GC11531
A long-acting β2-adrenergic receptor agonist
Cas No.:94749-08-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | The cells are rinsed twice with ice-cold phosphate-buffered saline and mechanically detached in ice-cold buffer containing 10 mM Tris·HCl, pH 7.4, 5 mM EDTA, 10 μg/mL benzamidine, 10 μg/mL soybean trypsin inhibitor (type II-S), and 5 μg/mL leupeptin (lysis buffer). The lysate is centrifuged at 45,000 ×g for 10 min at 4°C. The pellet is rehomogenized in lysis buffer, with a Potter-type homogenizer, and stored at −80°C until use. The competition binding assays are performed in buffer containing 75 mM Tris·HCl, pH 7.4, 12.5 mM MgCl2, and 2 mM EDTA, using 1-5 μg of membrane protein, 50 pM 125I-CYP, and 0-100 μM unlabeled ligand in the presence of 100 μM GTP, for 60 min at 37°C. The binding reaction is terminated by dilution and rapid filtration through Whatman GF/C filters; the filters are washed three times with solution containing 25 mM Tris·HCl, pH 7.4, and 1 mM MgCl2. Nonspecific binding is determined in the presence of 5 μM (±)-propranolol. The radioactivity on the filters is counted with a γ-counter. |
Animal experiment: | All mice are sensitized on days 0 and 14 by intraperitoneal injection of either PBS or 0.08 mg OVA and 0.1 mL aluminum hydroxide in 0.1 mL of PBS (pH 7.4). After sensitization, animals are exposed to aerosolized PBS-only (negative control), 1% OVS/PBS (acute exposure), 1% OVA/0.01% LPS/PBS (extra LPS exposure) or 1% OVA/0.01% LPS/salmeterol/PBS (sal treatment) for 40 min, once per day for 3 consecutive days (days 24-26). On day 27, the mice are killed and lungs are divided into two groups for analysis: the left lung lobes are lavaged three times with 1 mL of PBS with 1% fetal calf serum and 5 U/mL heparin, and the right halves are fixed by 4% paraformaldehyde for histological analysis. |
References: [1]. Sharma M, et al. Salmeterol; A Long Acting β2-Aderenergic Receptor Agonist Inhibits Macrophage Activation by Lipopolysaccharide From Porphyromonas Gingivalis. J Periodontol. 2017 Mar 3:1-17. | |
β2-adrenergic receptor agonists are a class of drugs acting on the beta2-adrenergic receptor, thereby causing smooth muscle relaxation, which results in dilation of bronchial passages, vasodilation in muscle/liver, relaxation of uterine muscle and release of insulin. Salmeterol xinafoate, as a long-acting beta2-adrenergic receptor agonist, is clinically prescribed for the treatment of asthma, chronic obstructive pulmonary disease (COPD) and other pulmonary disorders. It was previously marketed as a dry powder inhaler in the US and is still available in the UK market.
In vitro: In a previoius study, it was found that salmeterol could reduce retinal Müller cell death through the inhibition of the phosphorylation of IRS-1(Ser307). In addition, the findings also suggest the importance of IRS-1 in beta-adrenergic receptor signaling in the prevention of cell death in retinal Müller cells [1].
In vivo: A previous animal study showed that salmeterol significantly decreased the production of pro-inflammatory cytokines in a model of allergen-challenged mice, which expressed tumor-necrosis factor-alpha, interleukin-1 and interleukin-6. Moreover, it was found that salmeterol could reduce the inflammation caused by lipopolysaccharide in activated murine bone marrow-derived dendritic cells (DCs). Therefore, this study suggested that salmeterol regulated the inflammation of allergen-induced asthma by modulating DCs, providing evidence that DCs were the target immune cells responsible for the action of salmeterol against asthma [2].
Clinical trial: In an early clinical investigation, it was found that salmeterol was significantly better than disodium cromoglycate in improving both morning and evening PEF [3]. A recent Phase-2 clinical trial, named “Dose-Ranging Study of the Salmeterol Component of Fluticasone/Salmeterol Spiromax Compared to Fluticasone Spiromax and Advair Diskus in Asthma Subjects”, was conducted in the US to evaluate the dose response, efficacy and safety of salmeterol combined with fluticasone for the treatment of persistent asthma.
References:
[1] Walker RJ, Anderson NM, Bahouth S, Steinle JJ. Silencing of insulin receptor substrate-1 increases cell death in retinal Müller cells. Mol Vis. 2012;18:271-9
[2] Hu Z, Chen R, Cai Z, Yu L, Fei Y, Weng L, Wang J, Ge X, Zhu T, Wang J, Bai C. Salmeterol attenuates the inflammatory response in asthma and decreases the pro-inflammatory cytokine secretion of dendritic cells. Cell Mol Immunol. 2012;9:267-75.
[3] Bousquet J, Aubert B, Bons J. Comparison of salmeterol with disodium cromoglycate in the treatment of adult asthma. Ann Allergy Asthma Immunol. 1996;76:189-94.
| Cas No. | 94749-08-3 | SDF | |
| 别名 | 沙美特罗昔萘酸酯; GR 33343X xinafoate | ||
| 化学名 | 2-(hydroxymethyl)-4-[1-hydroxy-2-[6-(4-phenylbutoxy)hexylamino]ethyl]phenol;1-hydroxynaphthalene-2-carboxylic acid | ||
| Canonical SMILES | C1=CC=C(C=C1)CCCCOCCCCCCNCC(C2=CC(=C(C=C2)O)CO)O.C1=CC=C2C(=C1)C=CC(=C2O)C(=O)O | ||
| 分子式 | C36H45NO7 | 分子量 | 603.75 |
| 溶解度 | ≥ 30.1875 mg/mL in DMSO, ≥ 15.83 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
| 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 | 1.6563 mL | 8.2816 mL | 16.5631 mL |
| 5 mM | 0.3313 mL | 1.6563 mL | 3.3126 mL |
| 10 mM | 0.1656 mL | 0.8282 mL | 1.6563 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。