Olodaterol(BI-1744) hydrochloride

  Cat. No.:  DC9248   Featured
Chemical Structure
869477-96-3
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Field of application
Olodaterol is a novel, long-acting beta2-adrenergic agonist (LABA) that exerts its pharmacological effect by binding and activating beta2-adrenergic receptors located primarily in the lungs.
Cas No.: 869477-96-3
Chemical Name: (R)-6-hydroxy-8-(1-hydroxy-2-((1-(4-methoxyphenyl)-2-methylpropan-2-yl)amino)ethyl)-2H-benzo[b][1,4]oxazin-3(4H)-one hydrochloride
Synonyms: Olodaterol hydrochloride; Olodaterol HCl; BI-1744; BI 1744; BI1744; Olodaterol; Striverdi
SMILES: CC(C)(CC1=CC=C(C=C1)OC)NC[C@@H](C2=CC(=CC3=C2OCC(=O)N3)O)O.Cl
Formula: C21H27ClN2O5
M.Wt: 422.906
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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].
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[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 h.
In Vitro: 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]. 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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC9248 Olodaterol(BI-1744) hydrochloride Olodaterol is a novel, long-acting beta2-adrenergic agonist (LABA) that exerts its pharmacological effect by binding and activating beta2-adrenergic receptors located primarily in the lungs.
DC10384 Olodaterol Olodaterol (BI1744) is a long acting β2-adrenoceptor agonist with an EC50 of 1.4±0.08 nM.
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