1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. Olodaterol

Olodaterol (BI1744) is a selective, long acting β2-adrenoceptor2-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.

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Olodaterol Chemical Structure

Olodaterol Chemical Structure

CAS No. : 868049-49-4

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

Olodaterol (BI1744) is a selective, long acting β2-adrenoceptor2-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].

IC50 & Target

β2 adrenoceptor

0.1 nM (EC50)

In Vitro

Olodaterol (0.001~10 nM; fibroblasts) attenuates growth factor-induced motility and proliferation[2].
Olodaterol (0.1~10 nM; fibroblasts) interferes with FGF-induced phosphorylation of signalling cascades[2].
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.

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.
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[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

386.44

Formula

C21H26N2O5

CAS No.
Appearance

Solid

Color

Light yellow to khaki

SMILES

O=C1NC2=CC(O)=CC([C@@H](O)CNC(C)(C)CC3=CC=C(OC)C=C3)=C2OC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

H2O : 6.2 mg/mL (16.04 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5877 mL 12.9386 mL 25.8772 mL
5 mM 0.5175 mL 2.5877 mL 5.1754 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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
H2O 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

* 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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Olodaterol Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Olodaterol
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