Olodaterol|868049-49-4|(BI1744)-陌孚医药/Medlife

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Olodaterol (Synonyms: BI1744)

目录号: PL14300 纯度: ≥98%

CAS No. :868049-49-4

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PL14300-100mg	100mg	¥14218.18	请登录
PL14300-200mg	200mg	询价	询价
PL14300-500mg	500mg	询价	询价

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中文名称	Olodaterol
中文别名	6-羟基-8-[(1R)-1-羟基-2-[[2-(4-甲氧基苯基)-1,1-二甲基乙基]氨基]乙基]-2H-1,4-苯并恶嗪-3(4H)-酮;奥达特罗;6-羟基-8-[(1r)-1-羟基-2-[[2-(4-甲氧基苯基)-1,1-二甲基乙基]氨基]乙基]-2H-1,4-苯并噁嗪-3(4h)-酮;奥达特罗杂质
英文名称	Olodaterol
英文别名	6-Hydroxy-8-[(1R)-1-hydroxy-2-[[2-(4-methoxyphenyl)-1,1-dimethylethyl]amino]ethyl]-2H-1,4-benzoxazin-3(4H)-one;Olodaterol;6-hydroxy-8-[(1R)-1-hydroxy-2-[[1-(4-methoxyphenyl)-2-methylpropan-2-yl]amino]ethyl]-4H-1,4-benzoxazin-3-one;BI1744;Striverdi Respimat;Olodaterol Free Base;BI 1744;VD2YSN1AFD;Striverdi respimat (TN);Striverdi;6-Hydroxy-8-((1R)-1-hydroxy-2-((2-(4-methoxyphenyl)-1,1-dimethylethyl)amino)ethyl)-2H-1,4-benzoxazin-3(4H)-one;(R)-6-hydroxy-8-(1-hydroxy-2-((1-(4-methoxyphenyl)-2-methylpropan-2-yl)amino)ethyl)-2H-benzo[b][1,4]oxazin-3(4H)-one;Olodatero
Cas No.	868049-49-4
分子式	C₂₁H₂₆N₂O₅
分子量	386.44
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Olodaterol (BI1744) 是一种选择性、长效的 β₂-adrenoceptor (β₂-AR) 激动剂(EC₅₀=0.1 nM；pK_i= 9.14 for human β₂-adrenoceptor)。 Olodaterol 可用于慢性阻塞性肺疾病 (COPD) 和肺纤维化。

生物活性

Olodaterol (BI1744) is a selective, long acting β 2 -adrenoceptor (β 2 -AR) agonist (EC 50 =0.1 nM and pK i = 9.14 for human β 2 -adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis.

性状

Solid

IC50 & Target[1][2]

β2 adrenoceptor 0.1 nM (EC50)

体外研究(In Vitro)

Olodaterol (0.001~10 nM; fibroblasts) attenuates growth factor-induced motility and proliferation.
Olodaterol (0.1~10 nM; fibroblasts) interferes with FGF-induced phosphorylation of signalling cascades.
Olodaterol (0.001~1000 nM; 30 minutes; fibroblasts) increases intracellular cAMP in a concentration-dependent manner. Olodaterol (0~10 nM; 30 minutes; fibroblasts) concentration-dependently inhibits the PICP increase with maximal efficacy of 70 % at 10 nM. Olodaterol has a subnanomolar affinity for the β2-AR (pKi=9.14) and is selective for this receptorin comparison with the β1-AR and β3-AR subtypes. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Olodaterol (1 mg/kg; inhal.; 21 days) accelerats body weight recovery back to control levels (at day 21) and attenuats TGF-β-induced lung fibrosis.
Olodaterol (0.1~3 μg/kg; inhal.; 5 hours) induces a dose-dependent bronchoprotection.
Olodaterol (0.3 and 0.6 μg/kg; inhal.; 24 hours) induces a maximal bronchoprotection of approximately 60 % after 0.5 hours. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Xing G, et al. Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent β2-adrenoceptor agonists. Bioorg Med Chem. 2020;28(1):115178.
[2]. Herrmann FE, et al. Olodaterol shows anti-fibrotic efficacy in in vitro and in vivo models of pulmonary fibrosis. Br J Pharmacol. 2017;174(21):3848-3864.

溶解度数据	In Vitro: H₂O : 6.2 mg/mL (16.04 mM; Need ultrasonic and warming)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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