Art. -Nr.: HY-14301

Olodaterol

(Synonyms: BI1744)

2 Cited Publications

Kundenbewertung

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 pK_i= 9.14 for human β₂-adrenoceptor, respectively). Olodaterol can be used for chronic obstructive pulmonary disease (COPD) and pulmonary fibrosis.

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Reinheit: 99.85%
CAS. Nr.: 868049-49-4
Formel: C₂₁H₂₆N₂O₅
Molecular Weight:386.44

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Olodaterol Chemical Structure

CAS. Nr.: 868049-49-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

β2 adrenoceptor

0.1 nM (EC₅₀)

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

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 (pK_i=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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 868049-49-4
Appearance Solid
Molecular Weight 386.44
Formel C₂₁H₂₆N₂O₅
Color Off-white to yellow
SMILES

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

BI1744
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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
SSRN

2026 Apr 14.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5877 mL

12.9386 mL

25.8772 mL

5 mM

0.5175 mL

2.5877 mL

5.1754 mL

10 mM

0.2588 mL

1.2939 mL

2.5877 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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.

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) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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 / 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.

Keywords

Olodaterol

2 Cited Publications

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Olodaterol

NMPA-Approved Drug Library

Neurotransmitter Receptor Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Obesity Compound Library

Targeted Diversity Library

Antidepressant Compound Library

Protein-protein Interaction Inhibitor Library

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Human Metabolite Library

Anti-Pulmonary Fibrosis Compound Library

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Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

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Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Olodaterol

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Olodaterol

NMPA-Approved Drug Library

Neurotransmitter Receptor Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Obesity Compound Library

Targeted Diversity Library

Antidepressant Compound Library

Protein-protein Interaction Inhibitor Library

EMA-Approved Drug Library

Human Metabolite Library

Anti-Pulmonary Fibrosis Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

RNA Binding Bioactive Compound Library

Lactylation Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Olodaterol

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Olodaterol Related Classifications

HY-14301 Related Classifications