Salmeterol-d3 (xinafoate)
(Synonyms: GR 33343X-d3 xinafoate) 目录号 : GC48068
A neuropeptide with diverse biological activities
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Salmeterol-d3 is intended for use as an internal standard for the quantification of salmeterol by GC- or LC-MS. Salmeterol is a long-acting β2-adrenergic receptor agonist (β2-AR; EC50s = 0.79, 63.1, and 9.4 nM for β2-, β1-, and β3-ARs, respectively).1 It inhibits electrically-stimulated contraction of isolated guinea pig trachea strips (EC50 = 2.51 nM) and histamine-induced bronchoconstriction in guinea pigs via aerosol administration of doses ranging from 0.12 to 12 mM.1,2 Salmeterol binds to an exosite domain of β2-adrenergic receptors, producing a slow onset of action and prolonged activation.3 Formulations containing salmeterol have been used in the treatment of asthma, including exercise-induced asthma, and chronic obstructive pulmonary disease.
1.Procopiou, P.A., Barrett, V.J., Ford, A.J., et al.The discovery of long-acting saligenin β2 adrenergic receptor agonists incorporating a urea groupBioorg. Med. Chem.19(20)6026-6032(2011) 2.Ball, D.I., Brittain, R.T., Coleman, R.A., et al.Salmeterol, a novel, long-acting β2-adrenoceptor agonist: Characterization of pharmacological activity in vitro and in vivoBr. J. Pharmacol.104(3)665-671(1991) 3.Isin, B., Estiu, G., Wiest, O., et al.Identifying ligand binding conformations of the β2-adrenergic receptor by using its agonists as computational probesPLoS One7(12)e50186(2012)
| Cas No. | N/A | SDF | |
| 别名 | GR 33343X-d3 xinafoate | ||
| Canonical SMILES | OC([2H])([2H])C1=CC(C(O)([2H])CNCCCCCCOCCCCC2=CC=CC=C2)=CC=C1O.OC3=C(C(O)=O)C=CC4=CC=CC=C43 | ||
| 分子式 | C25H34D3NO4.C11H8O3 | 分子量 | 606.8 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 25 mg/ml,Ethanol: 2 mg/ml | 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 | 1.648 mL | 8.2399 mL | 16.4799 mL |
| 5 mM | 0.3296 mL | 1.648 mL | 3.296 mL |
| 10 mM | 0.1648 mL | 0.824 mL | 1.648 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。
Salmeterol xinafoate
Profiles Drug Subst Excip Relat Methodol 2015;40:321-69.PMID:26051688DOI:10.1016/bs.podrm.2015.02.002.
Salmeterol xinafoate is a potent and a long-acting β2-adrenoceptor agonist. It is prescribed for the treatment of severe persistent asthma and chronic obstructive pulmonary disease. Different methods were used to prepare (R)-(-)-salmeterol such as: mixing a sample of 4-benzyloxy-3-hydroxymethyl-ω-bromoacetophenone with sodium lauryl sulfate and the mixture was added to the microbial culture of Rhodotorula rubra, treatment of p-hydroxyacetophenone with Eschenmoser's salt and carbonate exchange resin followed by a sequence of supported reagents and scavenging agents or via Rh-catalyzed asymmetric transfer hydrogenation. The enantioselective synthesis of (S)-salmeterol was achieved via asymmetric reduction of the azidoketone 4 by Pichia angusta yeast. Physical characteristics of salmeterol xinafoate were confirmed via: X-ray powder diffraction pattern, thermal analysis and UV, vibrational, nuclear magnetic resonance, and mass spectroscopical data. Initial improvement in asthma control may occur within 30 min following oral inhalation of salmeterol in fixed combination with fluticasone propionate. Clinically important improvements are maintained for up to 12 h in most patients. It is extensively metabolized in the liver by hydroxylation, thus increased plasma concentrations may occur in patients with hepatic impairment.
Salmeterol xinafoate. A review of its pharmacological properties and therapeutic potential in reversible obstructive airways disease
Drugs 1991 Nov;42(5):895-912.PMID:1723379DOI:10.2165/00003495-199142050-00010.
Salmeterol xinafoate, like salbutamol (albuterol), is a saligenin derivative, and a selective beta 2-adrenoceptor agonist. It produces bronchodilation for at least 12 hours following inhalation of a single 50 micrograms dose. Salmeterol is intended for regular twice-daily treatment of reversible airways obstruction and not for immediate symptomatic relief, and when used in this manner, 50 micrograms twice daily is more effective than salbutamol 200 micrograms or terbutaline 500 micrograms administered 4 times daily, or individually titrated oral doses of theophylline in improving objective and subjective criteria of efficacy in patients with mild to moderate asthma. Salmeterol 100 micrograms inhaled twice daily may provide better control than the lower dose in patients with severe asthma. The long duration of effect of salmeterol makes it particularly suitable for treating patients with nocturnal asthma in whom it improves sleep quality. The place of salmeterol, like that of other beta 2-adrenoceptor agonists used regularly in the treatment of asthma, is being debated. Patients in need of regular beta 2-agonist therapy should also be regarded as candidates for inhaled corticosteroids to counteract underlying inflammation. Thus, salmeterol may be particularly useful in patients requiring regular treatment with beta 2-agonists for nocturnal asthma and results of trials in progress involving large numbers of patients are awaited with interest.
Salmeterol xinafoate (SX) loaded into mucoadhesive solid lipid microparticles for COPD treatment
Int J Pharm 2019 May 1;562:351-358.PMID:30935915DOI:10.1016/j.ijpharm.2019.03.059.
Chronic obstructive pulmonary disease (COPD) is one of the main health problems worldwide. It is characterised by chronic inflammation in the lungs that leads to progressive, chronic, largely irreversible airflow obstruction. The use of long-acting β agonists remain today the frontline treatment for COPD with the aim of minimizing side effects and enhancing therapeutic usefulness. To this purpose, in this paper, mucoadhesive solid lipid microparticles (SLMs) containing a long-acting β-2 agonist, Salmeterol xinafoate (SX) were prepared, characterised (size, z-potential, aerodynamic diameter, turbidimetric evaluations, drug loading and entrapping efficiency) and tested in a model of bronchial epithelial cells. It was demonstrated that the incorporation of SX into SLMs led to the production of particles suitable for inhalation and more efficient than the free molecule at increasing the cAMP expression in bronchial epithelial cells. In conclusion, the prepared systems, due to their aerodynamic behaviour and mucoadhesive properties, could improve the retention time of SX in the lung epithelium and its therapeutic effect, thus representing a good strategy for the treatment of COPD patients.
Solubility prediction of salmeterol xinafoate in water--dioxane mixtures
Int J Pharm 2001 Mar 23;216(1-2):33-41.PMID:11274804DOI:10.1016/s0378-5173(00)00694-3.
The mole fraction solubility of salmeterol xinafoate was determined in various concentrations of dioxane in aqueous binary mixture. Maximum solubility was observed in 90% v/v dioxane and solubility parameter of the solute was estimated from solubility peak equal to 24.99 MPa(0.5). The predicting capability of four different cosolvency models was also evaluated employing a five data point training set. The solubility data at other cosolvent concentrations were predicted using the trained models, with percentage average errors for 28 drug solubility data sets in water-cosolvent mixtures lying between 12.5 and 15.0%. Further predictive model is proposed for accurate solubility predictions based on a minimum number of experiments. The percentage average error where tested was 10.6%.
Salmeterol xinafoate: a review of its pharmacological properties and therapeutic potential in reversible obstructive airways disease
Allergol Immunopathol (Madr) 1992 Mar-Apr;20(2):72-84.PMID:1359777doi
Salmeterol xinafoate, like salbutamol (albuterol), is a saligenin derivative, and a selective beta 2-adrenoceptor agonist. It produces bronchodilation for at least 12 hours following inhalation of a single 50 micrograms dose. Salmeterol is intended for regular twice-daily treatment of reversible airways obstruction and not for immediate symptomatic relief, and when used in this manner. 50 micrograms twice daily is more effective than salbutamol 200 micrograms or terbutaline 500 micrograms administered 4 times daily, or individually titrated oral doses of theophylline in improving objective and subjective criteria of efficacy in patients with mild to moderate asthma. Salmeterol 100 micrograms inhaled twice daily may provide better control than the lower dose in patients with severe asthma. The long duration of effect of salmeterol makes it particularly suitable for treating patients with nocturnal asthma in whom it improves sleep quality. The place of salmeterol, like that of other beta 2-adrenoceptor agonists used regularly in the treatment of asthma, is being debated. Patients in need of regular beta 2-agonist therapy should also be regarded as candidates for inhaled corticosteroids to counteract underlying inflammation. Thus, salmeterol may be particularly useful in patients requiring regular treatment with beta 2-agonists for nocturnal asthma and results of trials in progress involving large numbers of patients are awaited with interest.