2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
Target:
β2 adrenoceptor:0.1 nM (EC50)
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[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]. Animal Model: Lung fibrosis C57BL/6 mice Dosage: 1 mg/mL Administration: Inhal.; 21 days Result: Accelerated body weight recovery back to control levels (at day 21) and attenuated TGF-β-induced lung fibrosis. Animal Model: Guinea Pigs Dosage: 0.1~3 μg/kg Administration: Inhal.; 5 hours Result: Induced a dose-dependent bronchoprotection. Animal Model: Dogs Dosage: 0.3 and 0.6 μg/kg Administration: Inhal.; 24 hours Result: Olodaterol (0.6 μg/kg) induced a maximal bronchoprotection of approximately 60 % after 0.5 hours.
In Vitro
Olodaterol (0.001~10 nM; fibroblasts) attenuates growth factor-induced motility and proliferation[2]. Olodaterol (0.1~10 nM; fibroblasts) interferes with FGF-induced phosphorylation of signalling cascades[2]. 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[2]. Western Blot Analysis[2] Cell Line: Fibroblasts Concentration: 0.1~10 nM Incubation Time: Result: Interfered with FGF-induced phosphorylation of signalling cascades. Cell Proliferation Assay[2] Cell Line: Fibroblasts Concentration: 0.001~10 nM Incubation Time: Result: Attenuated growth factor-induced motility and proliferation.
Kinase Assay
Cell Assay
Animal Administration
References
[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.
Return Policy
If you are in any way unsatisfied with your purchase, you may return any item(s) within 365 days of its original purchase date.
Please provide your Order Number in the email. We strive to reply to all email inquiries within one business day.
