Home Neuronal Signaling Adrenergic Receptor agonist Salmeterol

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Salmeterol Adrenergic Receptor agonist

Cat.No.S5527

Salmeterol (Astmerole, GR-33343X, SN408D) is a long-acting beta2-adrenergic receptor agonist with Ki value of 1.5 nM for WT β2AR and shows very high selectivity for the WT β2AR(β1Ki/β2Ki ratio of approximately 1500).
Salmeterol Adrenergic Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 415.57

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Quality Control

Batch: S552701 DMSO]83 mg/mL]false]Ethanol]83 mg/mL]false]Water]Insoluble]false Purity: 99.9%
99.9

Solubility

In vitro
Batch:

DMSO : 83 mg/mL (199.72 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 83 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 415.57 Formula

C25H37NO4

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 89365-50-4 -- Storage of Stock Solutions

Synonyms Astmerole, GR-33343X, SN408D Smiles C1=CC=C(C=C1)CCCCOCCCCCCNCC(C2=CC(=C(C=C2)O)CO)O

Mechanism of Action

Targets/IC50/Ki
β2-adrenergic receptor
(Cell-free)
1.5 nM(Ki)
In vitro
Salmeterol is highly lipophilic and diffuses through the lipid bilayer in muscle cell membranes to reach the β2-ARs, explaining its slow onset and long duration of action. This compound has been found to cause a dose-dependent increase in cAMP levels in neutrophils, an effect that is expected to reduce neutrophil-endothelial cell adhesion through inhibition of neutrophil Mac-1 cell surface expression.
In vivo
Salmeterol decreases the production of pro-inflammatory cytokines in a model of allergen-challenged mice that expressed tumor-necrosis factor-alpha, interleukin-1 and interleukin-6. This compound inhibits lipopolysaccharide-induced neutrophil recruitment to the lungs by a mechanism that possibly in part is mediated by an effect on neutrophil CD11b.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05085587 Unknown status
Bioequivalence|Asthma
Respirent Pharmaceuticals Co Ltd.|Becro Ltd.
 October 1 2021 Phase 1
NCT04503460 Recruiting
Asthma
Imperial College London|European Research Council
 July 23 2021 Phase 4
NCT03755544 Completed
Asthma|Chronic Obstructive Pulmonary Disease
Orion Corporation Orion Pharma
 January 16 2019 --

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