Batefenterol
Batefenterol Basic information
- Product Name:
- Batefenterol
- Synonyms:
-
- GSK961081;GSK-961081;GSK 961081;TD-5959;TD 5959;TD5959;BATEFENTEROL
- Batefenterol
- (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
- GSK-961081,Batefenterol
- GSK-961081(Batefenterol/TD-5959)
- Batefenterol, 98%, a novel muscarinic receptor antagonist and β2-adrenoceptor agonist
- Batefenterol(GSK961081)
- Carbamic acid, N-[1,1'-biphenyl]-2-yl-, 1-[3-[[2-chloro-4-[[[(2R)-2-(1,2-dihydro-8-hydroxy-2-oxo-5-quinolinyl)-2-hydroxyethyl]amino]methyl]-5-methoxyphenyl]amino]-3-oxopropyl]-4-piperidinyl ester
- CAS:
- 743461-65-6
- MF:
- C40H42ClN5O7
- MW:
- 740.24
- Product Categories:
-
- APIs
- Mol File:
- 743461-65-6.mol
Batefenterol Chemical Properties
- Boiling point:
- 948.3±65.0 °C(Predicted)
- Density
- 1.41±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:67.0(Max Conc. mg/mL);90.51(Max Conc. mM)
- form
- A crystalline solid
- pka
- 8.89±0.20(Predicted)
- color
- Light yellow to yellow
Batefenterol Usage And Synthesis
Uses
Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.
in vivo
In the guinea pig bronchoprotection 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). Batefenterol exhibits a rapid rate of clearance and short half-life[2].
IC 50
mAChR2; mAChR3
References
[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. DOI:10.1124/jpet.114.216861
[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 β? agonist (MABA) for the treatment of chronic obstructive pulmonary disease (COPD). J Med Chem. 2015 Mar 26;58(6):2609-22. DOI:10.1021/jm501915g
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