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Batefenterol

Catalog No. T7079 CAS 743461-65-6

Synonyms: GSK961081, TD-5959

Batefenterol (TD-5959) (GSK961081, TD-5959) is a muscarinic receptor antagonist and β2-adrenoceptor agonist. It displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor (Ki:1.4/1.3/3.7 nM).

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Batefenterol, CAS 743461-65-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 70.00
2 mg	In stock	$ 98.00
5 mg	In stock	$ 148.00
10 mg	In stock	$ 228.00
25 mg	In stock	$ 428.00
50 mg	In stock	$ 638.00
100 mg	In stock	$ 892.00
1 mL * 10 mM (in DMSO)	In stock	$ 248.00

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Purity: 98.4%

Purity: 97.94%

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Description	Batefenterol (TD-5959) (GSK961081, TD-5959) is a muscarinic receptor antagonist and β2-adrenoceptor agonist. It displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor (Ki:1.4/1.3/3.7 nM).
Targets&IC50	β2:3.7 nM (Ki, cell free), M3 (human):1.3 nM (Ki, cell free), M2 (human):1.4 nM (Ki, cell free)
In vitro	In competition radioligand binding studies at human recombinant receptors, Batefenterol displays high affinity for hM2 (Ki; 1.4 nM), hM3 muscarinic receptors (Ki: 1.3 nM) and hβ2-adrenoceptors (Ki: 3.7 nM). Batefenterol behaves as a potent hβ2-adrenoceptor agonist (EC50: 0.29 nM for stimulation of cAMP levels) with 440- and 320-fold functional selectivity over hβ1- and hβ3-adrenoceptors, respectively [1].
In vivo	In the guinea pig broncho-protection assay, inhaled Batefenterol produces potent, dose-dependent inhibition of bronchoconstrictor responses via MA (ED50: 33.9 μg/mL), BA (ED50: 14.1 μg/mL), and MABA (ED50: 6.4 μg/mL) mechanisms. Significant bronchoprotective effects of Batefenterol are evident in guinea pigs via MA, BA, and MABA mechanisms for up to 7 days after dosing[1]. In guinea pig isolated trachea expressing native muscarinic M3 and β2, Batefenterol produces smooth muscle relaxation through a dual mechanism involving competitive antagonism of the M3 receptor (EC50: 50 nM) and agonism of the β2 receptor (EC50: 25 nM). The combined effect on both muscarinic receptors and β2 receptors is more potent than either function working alone (EC50: 10 nM) [2].

Synonyms	GSK961081, TD-5959
Molecular Weight	740.24
Formula	C40H42ClN5O7
CAS No.	743461-65-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (135.09 mM)

H2O: < 0.1 mg/mL (insoluble)

References and Literature

1. Hegde SS, et al. Pharmacologic characterization of GSK-961081 (TD-5959), a first-in-class inhaled bifunctional bronchodilator possessing muscarinic receptor antagonist and β2-adrenoceptor agonist properties. J Pharmacol Exp Ther. 2014 Oct;351(1):190-9. 2. Hughes AD, et al. Discovery of (R)-1-(3-((2-chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate (TD-5959, GSK961081, batefenterol): first-in-class dual pharmacology multivalent muscarinic antagonist and β₂ agonist (MABA) for the treatment of chronic obstructive pulmonary disease (COPD). J Med Chem. 2015 Mar 26;58(6):2609-22.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library GPCR Compound Library Anti-Neurodegenerative Disease Compound Library Inhibitor Library Anti-Cancer Drug Library NO PAINS Compound Library Bioactive Compounds Library Max Anti-COVID-19 Compound Library Neuronal Signaling Compound Library

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Keywords

Batefenterol 743461-65-6 GPCR/G Protein Neuroscience Adrenergic Receptor AChR GSK 961081 mAChR inhibit Muscarinic acetylcholine receptor GSK961081 TD 5959 TD5959 Inhibitor TD-5959 GSK-961081 Beta Receptor inhibitor

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