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Olodaterol hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Olodaterol hydrochloride图片
CAS NO:869477-96-3
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
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。
Cas No.869477-96-3
别名盐酸奥达特罗,BI1744 hydrochloride
分子式C21H27ClN2O5
分子量422.9
溶解度Water : 250 mg/mL (591.16 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Olodaterol (BI1744) hydrochloride is a selective, long acting β2-adrenoceptor (β2-AR) agonist (EC50=0.1 nM and pKi= 9.14 for human β2-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis[1][2][3].

Olodaterol hydrochloride (0.1~10 nM; fibroblasts) interferes with FGF-induced phosphorylation of signalling cascades[2].Olodaterol hydrochloride (0.001~10 nM; fibroblasts) attenuates growth factor-induced motility and proliferation[2].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[2].

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[2].Olodaterol (0.1~3 μg/kg; inhal.; 5 hours) induces a dose-dependent bronchoprotection[3].Olodaterol (0.3 and 0.6 μg/kg; inhal.; 24 hours) induces a maximal bronchoprotection of approximately 60 % after 0.5 hours[3].

[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.
[3]. Bouyssou T, et al. Pharmacological characterization of olodaterol, a novel inhaled beta2-adrenoceptor agonist exerting a 24-hour-long duration of action in preclinical models [published correction appears in J Pharmacol Exp Ther. 2013 Jul;346(1):161]. J Pharmacol Exp Ther. 2010;334(1):53-62.