Olodaterol

SKU: orb1223805

Description

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.

Key Properties

• CAS Number: 868049-49-4
• MW: 386.4415
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₆N₂O₅
• SMILES: CC(C)(CC1=CC=C(C=C1)OC)NCC(C2=C3C(=CC(=C2)O)NC(=O)CO3)O
• Target: Adrenergic Receptor
• Solubility: H2O: 6.2 mg/mL

Bioactivity

• In Vivo:
  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:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BI1744 CL

Quick Database Links

Gene Symbol

Adrenergic Receptor