Olodaterol
Based on 2 publication(s) in Google Scholar
Olodaterol (BI1744) 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.
For research use only. We do not sell to patients.
- Purity : 99.85%
- CAS No.: 868049-49-4
- Formula: C21H26N2O5
- Molecular Weight:386.44
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Olodaterol
MoreAll Adrenergic Receptor Isoforms
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Biological Activity
Description
IC50 & Target
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β2 adrenoceptor 0.1 nM (EC50) |
In Vitro
Olodaterol (0.001~10 nM; fibroblasts) attenuates growth factor-induced motility and proliferation[2].
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Olodaterol (0.1~10 nM; fibroblasts) interferes with FGF-induced phosphorylation of signalling cascades[2].
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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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Fibroblasts
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Concentration:0.1~10 nM
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Incubation Time:
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Result:Interfered with FGF-induced phosphorylation of signalling cascades.
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Cell Line:Fibroblasts
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Concentration:0.001~10 nM
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Incubation Time:
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Result:Attenuated growth factor-induced motility and proliferation.
In Vivo
? 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lung fibrosis C57BL/6 mice
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Dosage:1 mg/mL
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Administration:Inhal.; 21 days
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Result:Accelerated body weight recovery back to control levels (at day 21) and attenuated TGF-β-induced lung fibrosis.
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Animal Model:Guinea Pigs
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Dosage:0.1~3 μg/kg
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Administration:Inhal.; 5 hours
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Result:Induced a dose-dependent bronchoprotection.
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Animal Model:Dogs
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Dosage:0.3 and 0.6 μg/kg
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Administration:Inhal.; 24 hours
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Result:Olodaterol (0.6 μg/kg) induced a maximal bronchoprotection of approximately 60 % after 0.5 hours.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 868049-49-4
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Appearance Solid
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Molecular Weight 386.44
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Formula C21H26N2O5
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Color Off-white to yellow
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SMILES
O=C1NC2=CC(O)=CC([C@@H](O)CNC(C)(C)CC3=CC=C(OC)C=C3)=C2OC1
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Synonyms
BI1744
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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J Pharm Biomed Anal
Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]2021 Feb 20:195:113870. PMID: 33453569 -
Solvent & Solubility
In Vitro:
H2O : 100 mg/mL (258.77 mM; Need ultrasonic and warming)
DMSO : 100 mg/mL (258.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.47 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.47 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocols
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Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
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Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
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Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
Purity & Documentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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 P [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O / DMSO | 1 mM | 2.5877 mL | 12.9386 mL | 25.8772 mL | 64.6931 mL |
| 5 mM | 0.5175 mL | 2.5877 mL | 5.1754 mL | 12.9386 mL | |
| 10 mM | 0.2588 mL | 1.2939 mL | 2.5877 mL | 6.4693 mL | |
| 15 mM | 0.1725 mL | 0.8626 mL | 1.7251 mL | 4.3129 mL | |
| 20 mM | 0.1294 mL | 0.6469 mL | 1.2939 mL | 3.2347 mL | |
| 25 mM | 0.1035 mL | 0.5175 mL | 1.0351 mL | 2.5877 mL | |
| 30 mM | 0.0863 mL | 0.4313 mL | 0.8626 mL | 2.1564 mL | |
| 40 mM | 0.0647 mL | 0.3235 mL | 0.6469 mL | 1.6173 mL | |
| 50 mM | 0.0518 mL | 0.2588 mL | 0.5175 mL | 1.2939 mL | |
| 60 mM | 0.0431 mL | 0.2156 mL | 0.4313 mL | 1.0782 mL | |
| 80 mM | 0.0323 mL | 0.1617 mL | 0.3235 mL | 0.8087 mL | |
| 100 mM | 0.0259 mL | 0.1294 mL | 0.2588 mL | 0.6469 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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