Arformoterol (tartrate)
(Synonyms: 酒石酸福莫特罗; (R,R)-Formoterol tartrate) 目录号 : GC42851
A β2-AR agonist
Cas No.:200815-49-2
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
Aformoterol is the (R,R)-enantiomer of the β2-adrenergic receptor (β2-AR) agonist formoterol . It selectively binds to β1- over β2-ARs (Kds = 2.9 and 113 nM, respectively) as well as β3-adrenergic, B2 bradykinin, neurokinin 1 (NK1) and NK2 receptors when used at concentrations up to 3 μM. Aformoterol induces cAMP accumulation in cultured human bronchial epithelial cells. Ex vivo, aformoterol (0.01-1,000 nM) induces dose-dependent relaxation of guinea pig tracheal strips precontracted with carbamoylcholine , ovalbumin, or histamine (pD2s = 8.4, 9.5, and 9.5, respectively). In vivo, aformoterol reverses histamine- and ovalbumin-induced bronchoconstriction in guinea pigs (ED50s = 1 and 40 nmol/kg, respectively). Formulations containing aformoterol have been used in the treatment of chronic obstructive pulmonary disease (COPD).
| Cas No. | 200815-49-2 | SDF | |
| 别名 | 酒石酸福莫特罗; (R,R)-Formoterol tartrate | ||
| Canonical SMILES | COC1=CC=C(C[C@@H](C)NC[C@H](O)C2=CC(NC=O)=C(O)C=C2)C=C1.OC([C@H](O)[C@@H](O)C(O)=O)=O | ||
| 分子式 | C19H24N2O4•C4H6O6 | 分子量 | 494.5 |
| 溶解度 | DMF: 12.5 mg/ml,DMSO: 25 mg/ml,PBS (pH 7.2): 2.5 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 | 2.0222 mL | 10.1112 mL | 20.2224 mL |
| 5 mM | 0.4044 mL | 2.0222 mL | 4.0445 mL |
| 10 mM | 0.2022 mL | 1.0111 mL | 2.0222 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。
Arformoterol tartrate in the treatment of COPD
Expert Rev Respir Med 2010 Apr;4(2):155-62.PMID:20406080DOI:10.1586/ers.10.16.
Some basic scientific data suggest that (S)-enantiomers of beta(2)-agonists have different and sometimes opposing effects to (R)-enantiomers. These data may explain the paradoxical response of the airways to the repeated, chronic administration of racemic beta(2)-agonists. Therefore, it is possible that the use of (R)-enantiomers of beta(2)-agonists may be an alternative option to reduce the risks of long-term administration of inhaled long-acting agents. Arformoterol is the (R,R)-enantiomer of formoterol. It is currently available for use as a nebulized solution of Arformoterol tartrate and is approved in the USA for twice-daily administration in patients with chronic obstructive pulmonary disease (COPD). Clinical trials in COPD patients have demonstrated that Arformoterol is as effective in improving lung function and symptoms as other available long-acting inhaled beta(2)-agonists. Moreover, its safety for long-term administration has been documented in this population. These findings indicate that Arformoterol is an effective option for patients with COPD who could benefit from sustained bronchodilation delivered through nebulization, and can be an alternative for patients who cannot use conventional inhaler devices, including metered-dose inhalers or dry-powder devices.
Arformoterol: (R,R)-eformoterol, (R,R)-formoterol, Arformoterol tartrate, eformoterol-sepracor, formoterol-sepracor, R,R-eformoterol, R,R-formoterol
Drugs R D 2004;5(1):25-7.PMID:14725487DOI:10.2165/00126839-200405010-00004.
Sepracor in the US is developing Arformoterol [R,R-formoterol], a single isomer form of the beta(2)-adrenoceptor agonist formoterol [eformoterol]. This isomer contains two chiral centres and is being developed as an inhaled preparation for the treatment of respiratory disorders. Sepracor believes that Arformoterol has the potential to be a once-daily therapy with a rapid onset of action and a duration of effect exceeding 12 hours. In 1995, Sepracor acquired New England Pharmaceuticals, a manufacturer of metered-dose and dry powder inhalers, for the purpose of preparing formulations of levosalbutamol and Arformoterol. Phase II dose-ranging clinical studies of Arformoterol as a longer-acting, complementary bronchodilator were completed successfully in the fourth quarter of 2000. Phase III trials of Arformoterol began in September 2001. The indications for the drug appeared to be asthma and chronic obstructive pulmonary disease (COPD). However, an update of the pharmaceutical product information on the Sepracor website in September 2003 listed COPD maintenance therapy as the only indication for Arformoterol. In October 2002, Sepracor stated that two pivotal phase III studies were ongoing in 1600 patients. Sepracor estimates that its NDA submission for Arformoterol, which is projected for the first half of 2004, will include approximately 3000 adult subjects. Sepracor stated in July 2003 that it had completed more than 100 preclinical studies and initiated or completed 15 clinical studies for Arformoterol inhalation solution for the treatment of bronchospasm in patients with COPD. In addition, Sepracor stated that the two pivotal phase III studies in 1600 patients were still progressing. In 1995, European patents were granted to Sepracor for the use of Arformoterol in the treatment of asthma, and the US patent application was pending.
Arformoterol tartrate in the treatment of bronchoconstriction in patients with chronic obstructive pulmonary disease
Drugs Today (Barc) 2009 Jan;45(1):3-9.PMID:19271027DOI:10.1358/dot.2009.45.1.1313983.
Arformoterol tartrate inhalational solution is a nebulized bronchodilator that has been approved for long-term, twice-daily maintenance therapy for bronchoconstriction in patients with chronic obstructive pulmonary disease (COPD). It is a single-isomer ([R,R]-formoterol), selective, long-acting, full beta(2)-agonist with affinity for both subtypes of beta-adrenergic receptor, and 2-fold higher affinity for the beta(2) receptor versus racemic formoterol. It is 1,000-fold more potent in receptor-binding affinity compared to (S,S)-enantiomer of formoterol. More than 2,000 COPD patients have participated in 16 completed clinical trials, including phase III pivotal and open-label trials to evaluate the efficacy and safety of Arformoterol at doses ranged from 15 to 50 microg. These studies demonstrated that treatment with Arformoterol significantly improved various lung function parameters, overall clinical status and ability to function, as well as significantly reduced COPD exacerbations and use of rescue medication. In terms of safety, Arformoterol was found to be well tolerated in doses up to 50 microg/day with no reports of significant clinical, laboratory or cardiovascular adverse events, such as changes in QTc interval or cardiac arrhythmias. Recent asthma literature has alluded to caution with the use of long-acting beta-agonists (LABAs) (except probably in combination with inhaled corticosteroids) citing possible increase in the risk of asthma-related mortality. However, there is no comparable data available with regards to the use of LABAs in COPD patients.
One-year safety and efficacy study of Arformoterol tartrate in patients with moderate to severe COPD
Chest 2014 Dec;146(6):1531-1542.PMID:25451347DOI:10.1378/chest.14-0117.
Background: Arformoterol tartrate (Arformoterol, 15 μg bid) is a nebulized long-acting β2-agonist approved for maintenance treatment of COPD. Methods: This was a multicenter, double-blind, randomized, placebo-controlled study. Patients (aged ≥ 40 years with baseline FEV1 ≤ 65% predicted, FEV1 > 0.50 L, FEV1/FVC ≤ 70%, and ≥ 15 pack-year smoking history) received Arformoterol (n = 420) or placebo (n = 421) for 1 year. The primary assessment was time from randomization to respiratory death or first COPD exacerbation-related hospitalization. Results: Among 841 patients randomized, 103 had ≥ 1 primary event (9.5% vs 15.0%, for Arformoterol vs placebo, respectively). Patients who discontinued treatment for any reason (39.3% vs 49.9%, for Arformoterol vs placebo, respectively) were followed for up to 1 year postrandomization to assess for primary events. Fewer patients receiving Arformoterol than placebo experienced COPD exacerbation-related hospitalizations (9.0% vs 14.3%, respectively). Twelve patients (2.9%) receiving Arformoterol and 10 patients (2.4%) receiving placebo died during the study. Risk for first respiratory serious adverse event was 50% lower with Arformoterol than placebo (P = .003). Numerically more patients on Arformoterol (13; 3.1%) than placebo (10; 2.4%) experienced cardiac serious adverse events; however, time-to-first cardiac serious adverse event was not significantly different. Improvements in trough FEV1 and FVC were greater with Arformoterol (least-squares mean change from baseline vs placebo: 0.051 L, P = .030 and 0.075 L, P = .018, respectively). Significant improvements in quality of life (overall St. George's Hospital Respiratory Questionnaire and Clinical COPD Questionnaire) were observed with Arformoterol vs placebo (P < .05). Conclusions: Arformoterol demonstrated an approximately 40% lower risk of respiratory death or COPD exacerbation-related hospitalization over 1 year vs placebo. Arformoterol was well-tolerated and improved lung function vs placebo. Trial registry: ClinicalTrials.gov; No.: NCT00909779; URL: www.clinicaltrials.gov.
Compatibility of Arformoterol tartrate inhalation solution with three nebulized drugs
Curr Med Res Opin 2007 Oct;23(10):2477-83.PMID:17784997DOI:10.1185/030079907X233106.
Objective: Arformoterol tartrate inhalation solution (15 microg/2 mL) is approved for the twice-daily, long-term maintenance treatment of bronchoconstriction in patients with chronic obstructive pulmonary diseases (COPD). This study assessed the chemical and physical compatibility of Arformoterol (15 microg/2 mL) with ipratropium bromide (0.5 mg/2.5 mL), acetylcysteine (800 mg/4 mL), and budesonide (0.25 mg/2 mL and 0.5 mg/2 mL). Methods: Immediately (T(0)) and 30 min (T(30)) after preparation, the admixtures were tested by visual inspection, pH measurement, and HPLC assay of each active component. Results: For all admixtures, no visible signs of change were observed. The pH of all admixtures at T(0) ranged from 4.82 to 6.40, which was within the range of individual drugs. For all admixtures, no unacceptable changes (less than 1% or 0.1 pH unit) in the pH values were observed within 30 min compared with the initial pH values in the admixtures, which met acceptance criteria of not more than (NMT) 10.0%. At both T(0) and T(30), the assay of each active component in all admixtures ranged from 98.3% to 101.4% compared to the assay in control samples, which met acceptance criteria of NMT 10.0%. In addition, no changes (less than 8%) in the assay of each active component at T(30) were observed compared to the initial assay values, which met acceptance criteria of NMT 10.0%. This study did not evaluate the clinical efficacy or safety of mixing Arformoterol in patients. Nor did the study assess the aerosol characteristics of these admixtures or any potential changes in drug output. Conclusion: The results demonstrated that Arformoterol was chemically and physically compatible with commercially available nebulized formulations of ipratropium bromide, acetylcysteine, and budesonide.