Olodaterol
(Synonyms: 奥达特罗,BI1744) 目录号 : GC44508
A selective β2-AR agonist
Cas No.:868049-49-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Olodaterol is a selective agonist of β2-adrenergic receptors (β2-ARs; EC50s = 97.7 and 2,725 nM for human β2- and β1-ARs, respectively). In vivo, olodaterol completely reverses acetylcholine-induced bronchoconstriction without cardiovascular side effects in guinea pigs. It also exhibits dose-dependent bronchoprotection in a beagle model of acetylcholine-induced bronchoconstriction for a period of 24 hours, indicating potential for once-daily dosing. Formulations containing olodaterol have been used to treat bronchoconstriction associated with chronic obstructive pulmonary disease.
| Cas No. | 868049-49-4 | SDF | |
| 别名 | 奥达特罗,BI1744 | ||
| Canonical SMILES | COC1=CC=C(CC(C)(C)N([H])C[C@H](O)C2=C(OCC(N3[H])=O)C3=CC(O)=C2)C=C1 | ||
| 分子式 | C21H26N2O5 | 分子量 | 386.4 |
| 溶解度 | DMF: 20 mg/ml,DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml,DMSO: 15 mg/ml,Ethanol: 1 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 | 2.588 mL | 12.94 mL | 25.8799 mL |
| 5 mM | 0.5176 mL | 2.588 mL | 5.176 mL |
| 10 mM | 0.2588 mL | 1.294 mL | 2.588 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。
Tiotropium/Olodaterol: A Review in COPD
Drugs 2019 Jun;79(9):997-1008.PMID:31119643DOI:10.1007/s40265-019-01133-w.
Tiotropium/Olodaterol (Stiolto® Respimat®; Spiolto® Respimat®) is an inhaled fixed-dose combination of the long-acting muscarinic antagonist tiotropium bromide (hereafter referred to as tiotropium) and the long-acting β2-adrenergic agonist Olodaterol. It is available in several countries, including the USA, Japan, China and those of the EU, where it is indicated for the long-term maintenance treatment of patients with chronic obstructive pulmonary disease (COPD). The efficacy of tiotropium/Olodaterol 5/5 μg/day in patients with COPD was evaluated in phase III or IV trials of 6-52 weeks' duration. Tiotropium/Olodaterol improved lung function to a greater extent than each of its individual components or placebo in 12- and 52-week trials. In 6-week trials, tiotropium/Olodaterol provided greater lung function benefits over 24 h than the individual components, placebo or twice-daily fluticasone propionate/salmeterol. Tiotropium/Olodaterol also demonstrated beneficial effects on health-related quality of life (HR-QoL), dyspnoea, inspiratory capacity, exercise endurance and the need for rescue medication. In an 8-week open-label trial, umeclidinium/vilanterol was superior to tiotropium/Olodaterol for the primary endpoint of trough forced expiratory volume in 1 s. The tolerability profile of tiotropium/Olodaterol was generally similar to that of the individual components. In conclusion, tiotropium/Olodaterol provides a useful option for the maintenance treatment of COPD, with the convenience of once-daily administration via a single inhaler.
Tiotropium/Olodaterol: A Review in COPD
Drugs 2016 Jan;76(1):135-46.PMID:26683033DOI:10.1007/s40265-015-0527-2.
Tiotropium/Olodaterol (Stiolto™ Respimat®, Spiolto™ Respimat®) is a fixed-dose combination of the long-acting antimuscarinic agent tiotropium bromide (hereafter referred to as tiotropium) and the long-acting β2-adrenoreceptor agonist Olodaterol delivered via the Respimat® Soft Mist™ inhaler. It is indicated for the maintenance treatment of airflow obstruction in adults with COPD. Several randomized, phase III studies of 6-52 weeks' duration evaluated the efficacy of once-daily tiotropium/Olodaterol in patients with GOLD stage 2-3 or 2-4 COPD. Tiotropium/Olodaterol maintenance therapy improved lung function to a greater extent than the individual components or placebo and provided clinically meaningful improvements in health-related quality of life and dyspnoea in 12- and 52-week studies. Tiotropium/Olodaterol consistently improved 24-h lung function in 6-week studies, providing greater benefits than the monotherapies, placebo or twice-daily fixed-dose fluticasone propionate/salmeterol. Inspiratory capacity and exercise endurance were also improved with tiotropium/Olodaterol following 6 or 12 weeks' treatment. The tolerability profile of tiotropium/Olodaterol in the phase III studies was generally similar to that of the component monotherapies. The most common adverse events and serious adverse events during 52 weeks' therapy were respiratory in nature, with COPD exacerbation, unsurprisingly, reported most frequently with tiotropium/Olodaterol and component monotherapies. Although additional data assessing the effect of tiotropium/Olodaterol on exacerbations and comparative studies with other recommended therapies are needed to definitively position tiotropium/Olodaterol, current evidence indicates that tiotropium/Olodaterol is a useful treatment option for patients with COPD.
Olodaterol for the treatment of asthma
Expert Opin Investig Drugs 2016 Jul;25(7):861-6.PMID:27170011DOI:10.1080/13543784.2016.1188078.
Introduction: Long-acting β-agonist (LABA)/inhaled corticosteroid (ICS) combinations are still the mainstay of asthma therapy but there is a pressing need to increase adherence to the prescribed treatment achievable in general by reducing the dose frequency. Consequently, there is considerable interest within the pharmaceutical industry in the discovery of once-daily β2-agonists (ultra-LABAs) to be used as a part of a combination therapy for treating asthma. Areas covered: The authors review the preclinical and clinical development of Olodaterol, a new ultra-LABA characterized by an improved selectivity for β2-adrenoceptors and a rather high intrinsic efficacy profile, in asthma. The clinical results were generated by 4 Phase 2 trials, which have enrolled 731 asthmatic patients. Expert opinion: The available results indicate that Olodaterol is able to induce an effective 24-h bronchodilation and is safe. However, one cannot formulate a solid conclusion on the best dose and/or dose frequency to be used in asthma because trials were not powered to assess the differences between doses and dose frequencies. Apparently, there is no Phase 3 trial planned or ongoing for Olodaterol monotherapy in patients with asthma and also no attempt to combine Olodaterol with an ICS, which is surprising.
Olodaterol for the treatment of chronic obstructive pulmonary disease
Am J Health Syst Pharm 2016 Aug 1;73(15):1135-43.PMID:27354040DOI:10.2146/ajhp150364.
Purpose: Published data on the pharmacology, pharmacokinetics, efficacy, and safety of the once-daily, long-acting β2-agonist (LABA) Olodaterol are reviewed. Summary: Olodaterol (Striverdi Respimat, Boehringer Ingelheim), a LABA with high selectivity for β2-adrenergic receptors, is indicated for the treatment of chronic obstructive pulmonary disease (COPD); the recommended dose is 5 μg, to be delivered once daily via the Respimat inhaler. In 48- and 6-week Phase III clinical trials of Olodaterol evaluating various lung function and symptomatic outcomes in patients with moderate to very severe COPD, Olodaterol use was associated with significant improvements in spirometry outcomes, such as postbronchodilator forced expiratory volume in one second (FEV1), as well as dyspnea severity and quality-of-life measures. Other clinical trials demonstrated that Olodaterol produced beneficial effects on FEV1 measures throughout the 24-hour dosing interval. A meta-analysis of data from 20 published research reports indicated that Olodaterol's efficacy was comparable to that of the once-daily LABA indacaterol and that the combination of Olodaterol and tiotropium provided improvements in lung function greater than those provided by tiotropium alone. Analysis of pooled data from four long-term trials showed that Olodaterol's safety profile was comparable to that of formoterol; the most frequently reported adverse effects associated with Olodaterol use were bronchitis, nasopharyngitis, and upper respiratory tract infection. Conclusion: Once-daily Olodaterol 5 μg is an effective therapy in improving lung function and symptomatic outcomes in patients with moderate to very severe COPD receiving other maintenance therapy, with a satisfactory safety profile.
Olodaterol for the treatment of chronic obstructive pulmonary disease: a narrative review
Expert Opin Pharmacother 2018 Oct;19(14):1603-1611.PMID:30311516DOI:10.1080/14656566.2018.1518431.
Inhaled bronchodilators are the key-stone of chronic obstructive pulmonary disease (COPD) management. Olodaterol 5 µg, a long-acting β2-adrenoceptor agonist (LABA) is one such bronchodilator indicated as a once-daily maintenance therapy. Areas covered: This article reviews the several trials that have assessed Olodaterol as a COPD therapy. It covers safety and tolerability data and provides the reader with an expert opinion on its use as a treatment for COPD. Expert opinion: Olodaterol improves lung function for 24 h and reduces rescue medication use. It may also improve dyspnea, exercise tolerance, and health-related quality of life. It is well tolerated with an acceptable cardiovascular and respiratory adverse event profile. There is some evidence that Olodaterol, as well as other LABAs, can reduce exacerbation frequency, but not FEV1 decline and death. LABAs alone are indicated in group A/B COPD subjects. Olodaterol and indacaterol are administered once-daily and may offer an adherence advantage over other LABAs with more frequent dosing schedules. Co-administration of an Olodaterol/tiotropium fixed dose combination in a single inhaler device is recommended as step-up in group A/B COPD subjects not sufficiently treated by Olodaterol alone or as initial therapy in those with severe exertional dyspnea.