| Name | Batefenterol |
| 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). |
| 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 100 mg/mL (135.09 mM)
H2O : < 0.1 mg/mL (insoluble)
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| Keywords | GSK 961081 | mAChR | inhibit | Muscarinic acetylcholine receptor | TD 5959 | Batefenterol | Adrenergic Receptor | TD5959 | Inhibitor | GSK-961081 | Beta Receptor |
| Inhibitors Related | Adiphenine hydrochloride | Nanofin | Arecoline hydrobromide | Forskolin | CLOZAPINE N-OXIDE | Pilocarpine nitrate | Ribavirin | Octopamine hydrochloride | Adenine | Choline chloride | Propoxur | Trazodone hydrochloride |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-COVID-19 Compound Library | Anti-Cancer Drug Library |
United States
