Olodaterol hydrochloride

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

Olodaterol Hydrochloride (BI1744 CL) 是一种有效的、选择性长效 β2 肾上腺素受体激动剂，对 hβ2 的 EC50 为 1.4 nM。

Olodaterol hydrochloride (BI1744 CL) is 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 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.(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.

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 miceDosage:1 mg/mL Administration:Inhal.; 21 daysResult: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 h.

BI1744 CL

GPCR/G Protein

Adrenergic Receptor

hβ2-adrenoceptor

Inflammation/Immunology

COPD

869477-96-3

413.895

C21H17ClFN3OS

>98% (HPLC)

DMSO: 50 mg/mL; Water: 15 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

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

4-(4-(4-fluorophenyl)-2-(4-(methylsulfinyl)phenyl)-1H-imidazol-5-yl)pyridine hydrochloride

(-20℃)

With Ice Pack

≥ 2 years