Olodaterol hydrochloride (Synonyms: BI1744 hydrochloride)
目录号: PL14277 纯度: ≥99%
CAS No. :869477-96-3
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中文名称
Olodaterol hydrochloride
中文别名
盐酸奥达特罗;奥达特罗盐酸盐
英文名称
Olodaterol hydrochloride
英文别名
Olodaterol Hydrochloride;6-hydroxy-8-[(1R)-1-hydroxy-2-[[1-(4-methoxyphenyl)-2-methylpropan-2-yl]amino]ethyl]-4H-1,4-benzoxazin-3-one,hydrochloride;Olodaterol hydrochloride
Cas No.
869477-96-3
分子式
C21H27ClN2O5
分子量
422.90
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Olodaterol (BI1744) hydrochloride 是一种选择性、长效的 β2-adrenoceptor (β2-AR) 激动剂 (EC50=0.1 nM;pKi= 9.14 for human β2-adrenoceptor)。 Olodaterol hydrochloride 可用于慢性阻塞性肺疾病 (COPD) 和肺纤维化。
生物活性
Olodaterol (BI1744) hydrochloride 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 hydrochloride (0.1~10 nM; fibroblasts) interferes with FGF-induced phosphorylation of signalling cascades.
Olodaterol hydrochloride (0.001~10 nM; fibroblasts) attenuates growth factor-induced motility and proliferation.
Olodaterol hydrochloride (0.001~1000 nM; 0.5 hours; fibroblasts) increases intracellular cAMP in a concentration-dependent manner. Olodaterol hydrochloride (0~10 nM; 0.5 hours; fibroblasts) concentration-dependently inhibits the PICP increase with maximal efficacy of 70 % at 10 nM. Olodaterol hydrochloride 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 weights 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
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 : 250 mg/mL (591.16 mM; Need ultrasonic)配制储备液
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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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