Olodaterol

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的长效 β2 肾上腺素受体激动剂，对 hβ2 的 EC50 为 1.4 nM；显示出比 hβ1 >250 倍的选择性；在没有全身药效作用的情况下，在狗和豚鼠中发挥支气管扩张作用超过 24 小时。

A potent, selective long-acting β2 adrenoceptor agonist with EC50 of 1.4 nM for hβ2; shows >250 fold selectivity over hβ1; exerts a bronchodilatory efficacy over 24 h in dogs and guinea pigs in the absence of systemic pharmacodynamic effects.COPD Phase 3 Clinical(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.(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.

Western Blot Analysis Cell Line:Fibroblasts Concentration:0.1~10 nM Incubation Time:Result:Interfered with FGF-induced phosphorylation of signalling cascades.Cell Proliferation Assay Cell Line:Fibroblasts Concentration:0.001~10 nM Incubation Time:Result:Attenuated growth factor-induced motility and proliferation.

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.

BI1744 CL

GPCR/G Protein

Adrenergic Receptor

β2-adrenoceptor

Inflammation/Immunology

COPD

868049-49-4

386.4415

C21H26N2O5

>98% (HPLC)

H2O: 6.2 mg/mL

CC(C)(CC1=CC=C(C=C1)OC)NCC(C2=C3C(=CC(=C2)O)NC(=O)CO3)O

2H-1,4-Benzoxazin-3(4H)-one, 6-hydroxy-8-[(1R)-1-hydroxy-2-[[2-(4-methoxyphenyl)-1,1-dimethylethyl]amino]ethyl]-

(-20℃)

With Ice Pack

≥ 2 years