Home Neuronal Signaling AChR antagonist - Adrenergic Receptor agonist Batefenterol 

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Batefenterol  AChR antagonist

Cat.No.S0032

Batefenterol (GSK961081, TD-5959) is both a muscarinic receptor antagonist and a β2-adrenoceptor agonist with Ki of 1.4 nM, 1.3 nM and 3.7 nM for hM2, hM3 muscarinic receptors and hβ2-adrenoceptor, respectively.
Batefenterol  AChR antagonist Chemical Structure

Chemical Structure

Molecular Weight: 740.24

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S003201 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.09%
99.09

Chemical Information, Storage & Stability

Molecular Weight 740.24 Formula

C40H42ClN5O7

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 743461-65-6 -- Storage of Stock Solutions

Synonyms GSK961081, TD-5959 Smiles COC1=CC(=C(C=C1CNCC(C2=C3C=CC(=O)NC3=C(C=C2)O)O)Cl)NC(=O)CCN4CCC(CC4)OC(=O)NC5=CC=CC=C5C6=CC=CC=C6

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (135.09 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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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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Mechanism of Action

Targets/IC50/Ki
hM3 muscarinic receptor [1]
(Cell-free assay)
1.3 nM(Ki)
hM2 muscarinic receptor [1]
(Cell-free assay)
1.4 nM(Ki)
hβ2-adrenoceptor [1]
(Cell-free assay)
3.7 nM(Ki)
References

Clinical Trial Information

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02064504 Completed
Pulmonary Disease Chronic Obstructive
GlaxoSmithKline
 February 19 2014 Phase 1
NCT00550225 Completed
Pulmonary Disease Chronic Obstructive
Theravance Biopharma|GlaxoSmithKline
 November 29 2007 Phase 1

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